TW386082B - 4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl [B] pyran-2-ones useful for treating infections due to HIV - Google Patents

Description

Amendment to the Chinese Application for Patent Application No. 83100644 (August 85) A7 B7 V. Description of the Invention (i >) (Please read the notice on the back to fill this page first) 匸 兵 54: 5776 Revealing Xiangdou * 3- (〇 (-Ethyl-para-methoxybenzyl) -4- 4-meryl. J48023942 (M 4-hydroxy-coumarin derivative-based rodenticide) and J. Labelled Compd Radiophare. 23 (2): 137-48, revealing 2H-1-benzopiperan-2-one, 4-hydroxy-7-methoxy-3- (bubenylpropyl) -OCA 107 ( 17): 154201f and CA 93 (23): 220546t. Example 7 4 compound (4-hydroxy-3- (1-phenyl-2-propenyl) -coumarin) is disclosed. CA 111 (13): 11138y CA 108 (15): 126707c; CA 107 (21): 1 93079s; CA 96 (19): 157432x; CA 93 (19): 181041c; CA 90 (l): 1707f; CA 88 (19): 132039w; CA 84 (9): 55338f; CA 79 (13): 74969a; and CA 71 (15): 69677j disclose the compound of Example 34 (4-hydroxy-3- [l- (l, 2,3,4-tetrahydro) Naphthyl] -coumarin) CA 79 (13): 74969a; CA 78 (7): 38016h; CA78 (7): 38016h; CA 78 (7): 38016h; CA 52: 5399b; CA 54 5699e; CA 54: 579e; and CA 72 (15): 78882v reveal that 4-hydroxycoumarin φ compounds are substituted at the 6- or 7-positions such as: methyl, methoxy and chlorine substitution > economy Consumption Cooperation with Employees of the Central Bureau of Standards of the People's Republic of China Du printed CA 54: 579e reveals the compound of Example 35 (4-hydroxy-3-Π-hydrofluorenyl] -coumarin). CA 63: 147 43c reveals the compound 4-hydroxy-3- (Bu Zekimethyl) _coumarin 0 r CA 63: 5589e reveals compound 3- (1 ·-(2-methoxy, 3-methyl, 5-chloro-phenyl) propyl) -4-hydroxy- Coumarin. _: __- 14.----- This paper size applies to China National Standard (CNS) A4 (210X297 mm) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 __B6___ V. Description of the invention (1 ) Field of the Invention The present invention is directed to compounds which can be used to inhibit retroviruses in human cells infected with retroviruses. More specifically, the present invention proposes 4-hydroxy-benzopiperan-2-one and 4-hydroxy-cycloalkyl [b] piperazine-2-hydrazone and its sulfonamide derivatives, and K is used as HIV-protein Qing inhibitor. BACKGROUND OF THE INVENTION Over the past decades, acquired immune deficiency micro-climates (AIDS) have evolved from the rare state of a rare individual's health to the problems of most people in the area of health and economics. John Saunders and Richard Storer, " New Developments in RT Inhibitors " DN & P 5 (3), April 1) 92, p 153-169. WHO figures show that over 360,000 cases of AIDSB have been published worldwide, including almost 175,000 cases. There are about 100,000 cases (50,000 cases in the United States) published in the world during the first 12 months. In the US painting, the number of seropositive carcasses is considered to be about 2 million. * It is estimated that the world has About 5-10 million are seropositive. Saunders and Storer, p 153 ° Since it was the disease described earlier in this decade *, the result of acquired immune deficiency microclimates (AIDS) and its reasoning is a constant theme and intensified reporting in popular and scientific journals . It is true that the compilation of Scientific African has been fully invested in AIDS (Scientific A dirty erica η 289, # 4 (1988)), and the literature on disease and abandonment is so huge Despise citations. On March 20, 1987, the FDA approved the use of Compound A AZT to treat and treat AIDS patients with the initial condition of recent carin pneumocystic pneumonia, without this condition {Please read the precautions on the back before writing this page) This paper scale 逯 肉 _ 圉 National Sample Standard (CNS) A4 Specification (2.10 Father 297 mm > Patent No. 831 00644 Patent Application Chinese Version Correction Sheet (August 1985) A7 B7 V. Description of Invention (Magic 7 ) And concentrated, and the residue was triturated with ether. The organic layer was washed with sodium bicarbonate aqueous solution, dried (magnesium acetate), and concentrated under reduced pressure. Flash chromatography on silica with 10% ethyl acetate / hexane was performed. 1.60 g of the title product was obtained as a colorless oil. Physical properties are as follows: AH NMR δ 1.31; 1.75; 2.65; 4.25; 7.04; 7.2; 7.49; 7.99 ° IR 2937, 1765, 1723, 1294, 1272, 1261, 1204, 1133, 1121 , 1082 cm-1. "-Analytical measured values: C, 73.37; Hf, 6.72. Example 2 4-hydroxy-3- (3-phenylpropyl) oligosine (formula A-5) is shown in Figure A. For 80 Mg of 60% sodium hydride / mineral oil in 3.0 ml of benzene, a suspension in a flame-drying flask, and 326 mg of the ester of preparation 2 were added under argon Liters of benzene solution. The mixture was refluxed overnight, then cooled and K methanol was stopped. The mixture was partitioned between acetic acid and 1N sodium hydroxide, and K was washed with 2 parts of ether. The aqueous layer was acidified to form a precipitate, and 4 parts of dichloride Methane-methyl ether extraction. The organic layer was condensed under reduced pressure and flash-chromatographed on silica with 50-70% ethyl acetate / hexane to give the title product of 108 mg of a white solid. Physical properties are as follows: Ministry of Economic Affairs Printed by the Consumer Standards Cooperative of the Central Bureau of Standards 隠 5 1.87; 2.63; 2.72; 7.2; 7.49; 7.87 ° 13C HHR δ 23.35, 29.46, 35.41, 104.94, 116.09, 116.16, 122.81, 123.51, 125.45, 128.02, 128.21, 131.06, 142.11, 151.97, 160.J3, 164.55 °

El HRMS [m] = 280.1102. Preparation 3 Ethylenediamine-Diacetic acid ______-S 9 -______ This paper rule applies to China National Standards (CNS) Person 4 Regulations Recruitment Plant (21 × 297 mm) Printed by A6, Consumer Cooperatives, Central Standards Bureau, Ministry of Economic Affairs B6 V. Description of the invention (2) The absolute CD4 lymphocyte number of patients with AIDS or virus-infected patients is less than 200 / mm3 in peripheral blood. AZT is a known inhibitor of viral reverse transcriptase, an enzyme necessary for human immunodeficiency virus replication. U.S. Patent 4.724,232 discloses a method for treating human acquired immune deficiency syndrome with 3'-®nitro-3'-deoxycytidine (AZT). After the discovery of AZT's anti-HIV live animals, more efforts were made to place more variety of dideoxynucleotide homologues, and K led to better effects. In the examples of 2, 3, and 2 deoxygenation series, ddC and ddl have been shown to antagonize HIV's potent activity in a test tube and have been evaluated in clinical trials. Saunders and Storer, p 160. The ddC compound is currently being developed by Hoffman-La Roche as a powerful anti-AIDS drug. Its limited toxicity in humans is peripheral neuropathy. This is recoverable at low doses. Raymond R. .Schinazi, Jan R. Mead and Paul M .. Feorino, " Insights Into HIV Cheeotherapy, " Aids Research and Huoan Retroviruses, Vo 1. .8, Hunber 6, 1992, p 963-990. PDA is licensed for use with AZT in the treatment of AIDS. The ddl compound has also been evaluated in bed tests. Its limiting toxicity is peripheral neuropathy and pancreatitis. It has also been shown to stimulate glycogenolysis of the liver and cause irreversible liver damage. Schinazi, Mead and Feorino, f > 966. It has recently been licensed by PqA for the treatment of adult and pediatric patients * whose HIV-infected AZT treatment is intolerable or whose health has been severely compromised. Schinazi, Mead and Feorino, p 966. Of these approved drugs, αΘτ is currently the only one that has been shown to reduce the mortality and frequency of infections associated with AIDS. Schin- This paper size applies to China National Standard (CNS) A4 specifications * (210x297 cm) ............... ............................................... ...... 、? · {Please read the precautions on the back before filling out this page} No. 83100S44 Patent Application Chinese Manual Correction Page (August 1985) = B7 V. Description of the invention (\ 士 3) Example of printing by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 71 3- (1 '-(3-bromophenyl) propyl) -4-hydroxycoumarin 4-hydroxycoumarin U98 mg) and bromo-1- (3-bromophenyl) propane (Preparation 39) (3.08 g) were placed in a capped vial under a nitrogen atmosphere in a 10010 oil bath. The mixture was heated to 175¾ at about 45 minutes, and the resulting melt was stirred at this temperature for 45 minutes, cooled to RT, diluted with M dichloromethane (45 ml), washed with water and brine (10 ml each), and sulfuric acid It was dried over sodium sulfate, and reduced to a residue under reduced pressure. The residue was chromatographed on silica gel (230-400 mesh sieve, 350 g), and dissolved in a gradient of ethyl acetate / hexane U5 / 85-60 / 40). The W TLC was pooled (ethyl acetate / curtin * 50/50) with fractions of Rf = 0.20 and the solvent was removed to give the title compound. The physical properties are as follows: Mp 168-172t :. Preparation 40 1- (4-Ethyloxyphenyl) propyl acetate (formula H-2) is shown in Figure Η. 1- (4-hydroxyphenyl) propionate (400 mg) in acetic anhydride (2 ml) The solution was added with pyridine (0.45 ml) under nitrogen. The solution was stirred at 01C for 30 minutes, then at RT for 2.5 hours, and then added to 1M hydrochloric acid (10 ml). The mixture M was extracted with dichloromethane (2 X 20 ml), and the mixed organic layer M was washed with brine (10 ml), dried over sodium sulfate, and concentrated under reduced pressure to give the title compound. The physical properties are as follows: CHN: found: C, 65,95; Η, 6.75. Example 72 3- (1 ·-(4-Ethyloxyphenyl ·) propyl) -4-hydroxycoumarin (formula Η-3) is shown in Figure Η 4-hydroxycoumarin (125 mg) and Europium carbonate (5 52 mg) in anhydrous B __-132 -___ This paper size applies to the Chinese national standard (CNS> Α4 size (210X297 mm) (Please read the notes on the back before filling in this page). Packing · Printed by A6 B6, Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs of the Pi Department of Economics. 5. Description of the invention (3) azi, Meadand F e 〇 ri ο, P 9 6 3 0 Identified as the causative agent of AIDS, but there are still a few opposing opinions (such as P. Duesberg,

Proc. Mati. Acad. Sci ’, USA, 86: 755-784 (1989)). Complete sequence analysis * of the genomes obtained from many infectious and non-infectious HIV-isolates has made the structure of the virus's suspicion, and the molecular forms necessary for its replication and maturation to the infectious form quite clear. HIV protein is necessary for processing the virus's gag and 838-? 1 polypeptide to modify it into mature virion protein. L. Ratner, et al., Nature, 313: 277-284 (1985); L.H. Pearl and W.R. Taylor,

Nature, 329: 351 (1987). HIV presents the same gag / pol / env as other retroviruses. L. Ratn.er, et al., Mature, 313 ^ 277-284 (1985) »S. Vain ~ Hobson, et al., Cell, 40: 9-17 (1985); R. Sanchez-Pescador, eta 1 , Science · 2 2 7: 4 8 4-4 9 2 (19 8 5); and MA Muesing. Et al., Mature, 313: 450-458 (1985) ° Reverse transcription plum (RT) is reverse transcription Viral enzymes catalyze the conversion of viral RNA to double-stranded DNA. AZT or other abnormal deoxynucleoside triphosphates are blocked at any point during the transcription process, making it impossible to prolong this point to cause playful results in terms of viral replication. Many studies have targeted RT targets, most of which are based on the ease of delivery of nucleosides of the AZT class to cells. However, due to the inadequacy of the tritiated to triphosphate step and the lack of specificity and sequential toxicity, the use of AZT and similar nucleosides with tritium-blocked or lost 3 'hydroxyl groups has suffered major setbacks . -5- This paper size applies to China National Sample Standard (CNS) A4 specification (210X297 mm) {Please read the precautions on the back before filling in this page)-Stapled by the Central Bureau of Standards, Ministry of Economic Affairs, Consumer Consumption Du printed A6 B6 V. Description of the invention (4) The T4 'cell receptor of HIV, the so-called CD4 molecule, has been regarded as the focus of invention in the treatment of 厶 105. 1 ?. Dian. 卩 丨 3} ^ ”, 6131., Nature, 331: 76-78 (1988); RE Hussey, et al .. Nature, 331: 78-81 (1988); and KC Deen, et al .. Nature, 331: 82-84 (1988). The outward part of this transmembrane protein is a 371 amino acid molecule (sCD4). It has been expressed in Chinese guinea pig egg cells (CHO), and Genentech ( DH Smith, et al., Science. 238: 1704-1707 (1987) > Naturally, the product was available in the second half of 1987 and was used in bed tests. CD4 has been shown to have a narrow activity against antagonistic viruses. Fan Hua, and so far cannot control human HIV infection. Schinazi, Mead and Feorino, P-963. The idea under CD4-based therapy is that molecules can be linked to T4 * by interfering with viruses and other Cells expressing CD4 on the surface can neutralize HIV. A variant of this subject is the adhesion of cytotoxins to CD4, K specifically binds and delivers to infected cells that present the glycoprotein gp-120 on their surface. M. Α Till, et al., Science, 242: 1166-1168 (1988); and VK Chaudhary, et al., Kature, 335 ^ 369-372 (1988) 〇 'Another treatment in AIDS Eyebrush has the inhibitory effect of prion protease. It is necessary to process the precursor of modified HI V-fusion polypeptide. In HIV and many other retroviruses, the proteolysis of gag and gag / pol fusion peptides into heat ( It is necessary to produce an infection f | viral particle. It has been shown that it is mediated by the protein plum * itself is coded by the P01 region of the viral genome. Y. Y 〇shinaka, eta 1 ., P r 〇c. N a 11. A cad. This paper is in accordance with the national standard (CNS) A4 specifications (210X297 mm) (please read the precautions on the back before filling in this page)-binding. Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 B6 r V. Description of Invention (5)

Sci. USA, 82: 1618-1622 (1985); Y. Yoshinaka, et al., J. Virol., 55 ^ 870-873 (1985); Y. Yoshinaka, et al., J. Virol., 57: 826-832 (1986); and K .. von der Hela, Proc. Hatl. Acad. Sci .. USA, 74 = 911-915 (1977). Inhibition of protein has been shown to inhibit the processing modification of HIV P5 5 in mammals and the replication of HIV in T lymphocytes. TJ HcQuade, et al., Science, 247 ^ 454 (1990) ° Protease, composed of only 99 amino acids, is the smallest known enzyme, and has been proven to be similar to asparagine plum, such as thin The homogeneity of protein seas and enzymes (L. H. Pear 1 and W. R. Tay 100r, Nature, 3 2 9: 3 5 1-354 (1987); and I. Katoh, et al , Nature, 329: 654-656 (1987)) The inference on the structure and mechanism of the three-dimensional space of enzymes has been experimentally supported (LH Pearl and WR Taylor, Nature, 329: 35, 354, 354 (1987)) Active HIV proteins have been expressed in bacteria (see, for example, PL Darke, et al., J. Biol. Chem., 264: 2307-2312 (1989 >) and chemically synthesized (J. Schneider and SB Kent, Cell, 54 * -363-368 (1988); and RF Nutt etal, P.r'o e. Natl. Acad. Sci., USA, Λ '. * 85: 7129-7133 (1988)). Mutation effects of position instructions (PL Darke, et al., J. Biol. Chen., 264: 2307-2312 (19 8 9); and N. E. Koh 1, eta 1., Proc, H a 11 A cad. Sci., USA, 85: 4686-4690 (1988)) and prion inhibitor Action (P.L.Darke, eta1., J.Bi ο1.Chem., 2 6 4: 2307-2312 (1989); S. Seel 丨 eier, et al., Proc. -7- The paper size is applicable to China National Standard (CNS) A4 specifications (210x297g ¢) (please read the precautions for back ruthenium before filling out this page). Binding printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. Invention description (6)

Hatl. Acad. Sci., USA, 85: 6612-6616 (1988); C.-Z. Gia · and I. Borsos · J. Biol. Che ·., 263: 14617-14720 (1988); and J. Hansen, et al., EMBO J., 7: 1785-1791 (1988)) has provided evidence for the effects of HIV proteases such as asparagus limboprotein-based seawater control. One study has demonstrated that the protease dissociates at the expected location in the peptide design. This occurs when the region is indeed dissociated by enzymes in the sag and pol pro-parent proteins during viral maturation. P.L.Darke, et al., Biochem. Biophys. Res. Communs .. 156: 297-303 (1988). X-ray crystallographic analysis of HIV protease (M.A. Navia, et al., Nature, 337: 615-620 (1989) and phase-directed reverse transcription from Lloyd's sarcoma virus (M.

Mil 1'er, et al, Nature, 337: 576-579 (1989)) show active positions in protein dimers. This is the same as seen in other aspartate proteases and therefore supports HI It is speculated that the V enzyme K dimer is only active (L. H. Pear 1 and W. R. Tay 100, Nature, 329: 351-354 (1987)). See also Joseph A. Martin, " Recent Advances in the Design of HIV Proteinase Inhibitors, " Antiviral.'Research, 17 (199.2) 265-278 And scientific research on safety methods, and thus make it possible to effectively treat diseases caused by this virus, such as acquired immunodeficiency syndrome (AIDS) »data reveals the synthesis of hybrids. XV. 4-Hydroxy-2-piranopyridines. E. -8- This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) (please read the precautions on the back before filling in this page)-binding and binding. A6 B6 Staff of Central Bureau of Standards, Ministry of Economic Affairs Printed by Consumer Cooperatives V. Description of Invention (7) Ziegler, H. Junek, and E. Nolken, Honatsh., 89: 678-82 (1958) (CA 53: 12283-4) reveals the following compound: 1-cyclooctane Ene-1-acrylic acid, α-benzyl-jS-2-dihydroxy-δ-lactone (CA 53: 12283i); hydrogenated cinnamic acid · "-[hydroxy (2-hydroxy-1-cyclopentene-butyl ) Methylene] 3 -endo (CA 53: 12283f); 1-cycloheptene-acrylic acid, α-benzyl-ling, 2-dihydroxy-3-lactone (CA 53: 12283h); Cyclodecene-acrylic acid * ot -benzyl- / 3, 2-dihydroxy-3 -endo (CA 53: 12283h); 1-cyclodecene-acrylic acid, < x-benzyl-fluorene, 2 -Dihydroxy-lactone (CA 53: 12284d). R. Effenberberger, T. Ziegler, R.-H. Schonwal-der, T. Kesaarszky, B. Bauer, Chen. Ber 119: 3394-3404 (1986), revealing cynanone intermediates such as compounds of formula Jl (wherein n is 4; see Scheme J below). Monatsh. Chem., 119 (6-7): 727-37 (1988) (CA 110 (13): 11443010 reveals compound 8H-) g and [1,2-b] piperan-8-fluorene, 10-hydroxyl -9- (benzylmethyl; and pyrene [2, 1-b] piperan-3 (5H) -one * 1-hydroxy-2- (phenylmethyl)-. CA 54: 14239b discloses compound W -2-Acrylic acid, α-benzyl- / 9, 3-dihydroxy-3 -endo. Monatsh. Chen., 113 (4): 475-84 (1982) revealed the compound piperano [2..3- c] pyrrole-2,5-dihydrazone, 6,7-dihydro-4-hydroxy-6- (3-methylphenyl) -7-benzyl-3- (benzylmethyl)-; and piperazine Furo [2,3-c] pyrrole-2,5-difluorene, 6,7-dihydro-4-hydroxy-6,7-diphenyl-3- (phenylmethyl)-. {Please Please read the notes on the back before filling in this page)-Binding. Staple. This paper size applies to China National Standard (CNS) A4 specification (210x297 mm). Printed by A6 __B6_ of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Explanation (8) CA 54: 14238h reveals compound 5H-benzocycloheptene-8-acrylic acid * α-benzyl-6,7-dihydro-cold, -9-dixiangyl-, δ-endoic acid. CA 54: 14238 & compound coumarin, 3-benzyl-5,6,7,8-tetrahydro-4-hydroxy_δ-isopropyl-5-methyl-. 〇 八 71 (21 >: 1016550 reveals the compound coumarin, 3-benzyl-5,6,7,8-tetrahydro-4-hydroxy. WO 8804652 (British equivalent AU 8810440) shows compound 2Η-1 -Benzopiperan-2-one, 3- (4-air-2-nitrobenzylglycolyl) -5.6,7,8-tetrafluoren-4-yl group. CA 55: 27296d reveals compound coumarin, 3- (3,5-Dimethylsalicyl) -5,6,7, _8-tetrahydro-4 -carboxyl-. CA 94 (9): 65472r 掲 shows 2-H-cyclooctyl [1 >] Piperidin-2-one · 5,6 · 7,3-hexahydro-3-phenyl; and heptyl [b] piperan-2 (5H) -fluorene, 6,7,8,9-tetrahydro- 4-Hydroxy-3-phenyl-. CA 59: 15185e reveals the compound Hexane diacid * 2-[hydroxy (2-hydroxy-bucyclopentene-butyl) methylene]-, δ-lactone.

Antiβicróbia 1 Patent Fast-Alert, Week Ending 30 April 1993, showing that cyclic amidines and homologues can be used as reverse transcription protease inhibitors. Summarized references are: CA 54: 577e (1960); CA 53: 12305e (1959); CA 51: 4826f, h (1957); CA 52: 5480g. H (1958); CA 51: 14827a: b (1957); and CA 51: 16453a (1957)-the compound of Example 10 (4-hydroxy-3- (1-phenylbutyl) -Pantholin example 11 compound (4-hydroxy-3- ( 1-Phenylpentyl) -coumarin> of -10- This paper has a small size and a standard (where) Η specifications (210X297 g 変) (Please read the precautions on the back before filling in this page) Printed by the Consumers' Cooperative of the Ministry of Standards and Standards of the People's Republic of China _____B6 _ V. Description of the Invention (9) Method; its use as a rodenticide; and its ability to reduce prothrombin in the blood. CA 54: 5699d ( 1960); CA 16450f (1960); and CA 53: 22454a (1959) showing the production method of 4-hydroxy-3- (1-phenylbutyl) · coumarin and its use as an anticoagulant and agricultural用法 usage.

Merch Index, 11 (1989), Entry 9950 * Warfarin, its chemical name --3-ex-phenylethyl. Brevylethyl-4-Xiangji crocetin--and its preparation Use of rodenticides and anticoagulants. J. Med. Chen., 1978, Vol. 21, Ho. 2: 231-234, showing the anti-vitamin K activity of warfarin and discussing the anticoagulant activity of many 3-substituted 4-hydroxycoumarins , Such as 4-hydroxy-3- (1-phenylbutyl) -myristotin. CA 55 ·· 22306β (1961) discusses the analysis of warfarin and absolute eaves type * and reveals the production method of 4-hydroxy-3- (buphenylbutyl) -myristole. AIDS 1993, Vol. 7, No. 1, ρ 129-130, discussing the role of warfarin in HIV-1 replication and expansion. CA 54: 577e (1960) discloses the preparation of a compound (3- (hexylphenylmethyl) -4-hydroxycoumarin).

Journal of Label led Compounds and Radiopharm-aceuticals, Vol. XXIII, Ho. 2: 137-148 (1986), showing the decrees and phenylpropanone, many deuterium-labeled metabolites, such as the deuterium tritium compound of Example 88 Note the same article (coumarin, 4-hydroxy-7-methoxy-3-U-phenylpropyl)-). J. Med. Chea. 21 (2): 23b 4 (1978); and J48023942 show the compound of Example 6 (4-hydroxy-3-((z-methylbenzyl) -coumarin) and its effect Use of rat medicine. -11 * • i: 'This paper rule) ϊ Applicable to National Standard (CNS) Sub 4 Specification (21〇x297 / h ^-Please read the precautions on the back before filling this page)-装 · 、 町. Consumption cooperation between employees of Zhongli Standards Bureau, Ministry of Economic Affairs, printed A6 _B6_ V. Description of invention (10) T r. Voronezh. Teckhno 1. Inst. 19 (2): 27-30 (1971), Abstract Ho Izh274 (Russian) shows the compound of Example 1 (4-hydroxy-3-phenethylcoumarin).

Helv. Chin. Acta 74 (7): 145 Bu 8 (1991); and Tr. Voronezh. Teckhnol. Inst. 19 (2) 5 27-30 (1971), Abstract Ho. Izh274 (Russian) discloses the compound of Example 2 (4-¾yl-3- (3-phenylpropyl) coumarin). J. Org. Chera. 33: 437-8 (1968); and Eur. J. Med. C hea.-C him T her. 12 (2): 12 5-3 0 (19 7 7) Example 7 Compound (4-hydroxy-3-diphenylmethylcoumarin). U.S. 3.764,693 shows the compound of Example 8 (4-Rhydryl-3- (3-syl-p-phenylbutyl) -coumarin) and its anticoagulant and rodenticide activity. CA 51: 577e shows the compound of Example 9 (4-hydroxy-3- (2-methyl-1-phenylpropyl) -coumarin). J48023942 (1973) discloses the compound of Example 14 (4-hydroxy-3- ( 3-methyl-1-benzylbutyl) -coumarin). CA 54: 16450f. Compound of Example 5 (4-Cyclo-3- (2-phenylpropyl) coumarin). '0 Ran 54: 5778 discloses the compound of Example 16 (4-Riyl-3- (1,3-diphenyl.ylpropyl) -coumarin). CA 54: 577e shows the compound of Example 18 (4-hydroxy-3- (1- (4-methylphenyl) butyl) -coumarin). J. Med. Chen. 18 (5 >: 513-19 ( 1975); and J. Chronatogr · 338 (2) · 325-34 (1985) 掲 Shi Bao Example 85 Compound-12- This paper size applies the Chinese National Standard (CNS) _A4 specification (21QX297 mm) '.. ........................................ ........ r .............................................. .. < Please read the notes on the back before filling out this page) A6 B6 dg3 = T ^ w Printed by the consumer cooperation of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (11) (Myristotin, 4-hydroxyl -3- [l- (4-hydroxyphenyl) propyl] _). CA 52: 5480h shows the compound of Example 20 (4-hydroxy-3- (1- (1-phenyl) -propyl) -myristole). J. Chronatogr. 562 U-2): 3, 8 (1991); and J. Labelled Coapds. Radiopharm. 23 (2); 137-48 (1986) shows the compound of Example 89 (coumarin, 4-hydroxy-6 -Methoxy-3- (1-phenylpropyl)-). J. Med. Che ·. 18 (5): 513-19 (1975); and J. Chronatogr. 529 (2): 479-85 (1990) Examples of compounds 93 and 95 are shown, (myristotin, 4,7-dihydroxy-3- (1-phenylpropyl) _ and coumarin, 4,6-diisopropyl-3- ( 1-phenylpropyl CA 54: 5699d; and CA 54: 577h show Example 90 also a compound (myristole, 4-hydroxy-7-methyl-3-(1-phenylpropyl)-). CA 54 : 577h shows the compound of Example 92 (myristotin, 7-chloro-4-hydroxy-3-U-phenylpropyl)-). CA 54: 577e shows the compound of Example 94 (fraxin, 4-hydroxy-3- [l- (4-methoxyphenyl) propyl]-). J. Med. Che ·. 18 (5>: 513-19 (1975) discloses Example 103 Compound (coumarin * 4-hydroxy-3- [l- (3-hydroxyphenyl) propyl]-). CA 54: 577f and CA 53: 20046a show the compound of Example 36 (Myristotin, 3-(. α ethyl-para-fluorobenzyl)- 4-hydroxy-). J. C hr 〇at 〇gr. 5 6 2 (1-2): 31-3 8 (19 91), and Arch, Environ. Conta .. Toxicolo. 14 (1): 111-129 < 1985> indicates para-chlorophenylpropanone. -13- This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) ) (谙 Please read the precautions on the back before filling this page)-Binding. Binding Amendment No. 83100644 Patent Application Revision Chinese Manual Correction Page (August 1985) A7 B7 V. Description of Invention (i >) (Please read the back first Cautions on this page fill in this page) Bing 54: 5776 reveals coumarin * 3- (〇 (-ethyl-para-methoxybenzyl) -4-meridian. J48023942 (M 4-hydroxy -Coumarin derivative-based rodenticide) and J. Labelled Compd. Radiophare. 23 (2): 137-48, revealing 2H-1-benzopiperan-2-one, 4-hydroxy-7- Methoxy-3- (bubenylpropyl) -OCA 107 (17): 154201f and CA 93 (23): 220546t Revealed Example 7 4 Compound (4-hydroxy-3- (1-phenyl-2- Allyl) -coumarin). CA 111 (13): 11138y; CA 108 (15): 126707c; CA 107 (21): 1 93079s; CA 96 (19): 157432x; CA 93 (19): 181041c; CA 90 (l): 1707f CA 88 (19): 132039w; CA 84 (9): 55338f; CA 79 (13): 74969a; and CA 71 (15): 69677j disclose the compound of Example 34 (4-hydroxy-3- [l- (l, 2,3,4-tetrahydro) naphthyl] -coumarin). CA 79 (13): 74969a; CA 78 (7): 38016h; CA78 (7): 38016h; CA 78 (7): 38016h; CA 52: 5399b; CA 54: 5699e; CA 54: 579e; and CA 72 ( 15): 78882v Reveals 4-hydroxycoumarin φ compound, which is substituted by 6- or 7-position such as: methyl, methoxy and chlorine > employee consumption cooperation of Central Standard Bureau of Ministry of Economic Affairs 54: 579e discloses the compound of Example 35 (4-hydroxy-3-Π-hydrofluorenyl] -coumarin). CA 63: 147 43c reveals compound 4-hydroxy-3- (buzekiylmethyl) _coumarin 0 r CA 63: 5589e reveals compound 3- (1 ·-(2-methoxy, 3-methyl, 5-methyl Chloro-phenyl) propyl) -4-hydroxy-coumarin. _: __- 14.----- This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) tgsig »Printed by A6 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs _B6_ V. Description of the Invention (13) CA 64: 12969b discloses compound 3- (α-propionyl-α-ethoxybenzyl) -4-hydroxy-coumarin. CA 83 (5): 37913 4 reveals compound 2H-benzobenzopyridin-2-one · 4-hydroxy-3-: 1- (3- (phenylmethoxy) phenyl] propyl]-. LR P'hl, Synthesis and Thin-Layer Chromatogaphic, Ultraviolet, and Mass Spectral Properties of the Anticoagulant Phenprocoumon and Its Honohfdroxylated Derivatives, J. Med. Chem. 18 (5): 513 519 (1975), showing the compound 4-hydroxy-8 -(Phenylmethoxy) -3- (1- 5ylpropyl) -2H-: l-benzopiperan-2-fluorene. JM Kider, United States Patent Ho. 3,835,161 · September 10, 1974 Japan, exemplified compound 3- [1- [4- (2-bromoethyl) phenyl] ethyl] -4-hydroxy-2H-] benzopiper-2-_. J0 3227 923-A (Sawai (Seiyaku KK) discloses the use of coumarin as a therapeutic agent for patients with systemic dysfunction; however, unsubstituted 4-hydroxypumarol is the only compound for this purpose & will be disclosed separately. WO 91 / G i363 (Univ. of Calif, at Oakland), sincerely on April 18, 1991, showing 6-Poly "1,2-benzopiperane" can be used to treat viral diseases. W0 91/1 304 (Kabi Pharmaceutical), published Announced the use of H-phenyl-H-methyl-1,2-di 4-Hydroxy-1-methyl-2oxy-pyridoline-3-curamidamine, also known as Linomide®, for the treatment of anti-recorded virus infections. Interprofessional Case No. WO 8 & / 07939 , Published on September 8, 1989 (please read the precautions on the back before filling in this page) /-\ -d-. Binding. Binding. -15-, · This paper is applicable to the standard: ϋ 准 ( CiiS) 酽 4 Specification (210x297 public love) No. 83100644 Patent Application Chinese Manual Revision Page U5 Aug. 5) A7 B7 V. Invention Description (/ ^ /) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, revealing the unique Coumarin compounds, which are reverse transcriptase inhibitors. J. Heterocyclic Chen. 23: 87-92 (1986) shows the synthesis of substituted coumarins, including 3-hydroxycoumarin. U.S. Patent No. 4,382,951 discloses clumsiness The benzopiperan and benzothiopiperan derivatives are not substituted with a hydroxyl group at the 4-position or are not substituted with a carbonyl group at the 2-position, and have antibacterial activity. U.S. Patent No. 3,489,774, Friends' 3,493,586 discloses that 3-(/ 3-aryl- / 3- (arylthio) (or arylselenium) propionylcoumarin, and piperidine products can be used as parasiticides Insecticides: Biochemical and Biophysical Research Coromunica-tions, Vol. 188, Ho. 2, 1992, p 631-637, revealing that the chromoone (Scutellaria baicalensis) with hydroxy substituent and phenol group is spread at the 2-position. Anti-HIV-1 protease activity. Antimicrobial Patent Fast-Alert, Week Ending 4 September 1992 * Reveals α-piperone, •-% azul, and ττ ** thio-vibram, which can be used as antiviral agents. International patents Hos. WO 92/04326 * 92/04327 and 92/04328, both published on March 19, 1992, disclose antiviral heterocyclic derivatives, such as B-quinoline and benzopiperanone, Acts as a replication inhibitor K for herpes type 1 and 2 * cytomegalovirus and Epstein-Barr virus. CA Selects: Antitumor Agents, Issue 19, 1992, 25, ^ 〇.1 17-901479 (-(: 1'International Patent case "0 92 06,687" discloses 5-iodo-5-amino-1,2-benzopiperan and its homologues, which can be used as cytostatic and antiviral agents. (Please read the back page first Note ^ phen ^ fill this page)..,? Line--: ----- ---- 2 ~~-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) No. 83100644 Revised page of Chinese specification of patent application (δ_1985) A7 ____B7 V. PCT published under the description of invention (ft) M reveals peptides that can be used as retroviral protein plum inhibitors: International Case No. W0 91 / 06561, published on May 16, 1991; and International Case No. W0 92/17490, published on October 15, 1992 0 W0 93/07868 * Published on April 29, 1993 reveals new nitroso- Benzofuranone, -benzylamine and -isoquinol derivatives, can be used as adenosine diphosphate diribosyltransferase inhibitors to treat viral infections and cancers. W0 93/07128, published April 1993-April 15 It is a substituted cyclic carbonyl group and its derivatives, which can be used as „retroviral protease inhibitor 0 J. Indian Chen. Soc. 69: 397-398 (July 1992), revealing couma beans 4-4-acetic acid was screened for its anti-cancer and anti-AIDS activities and was found to be inactive.

The Journal of Antibiotics, 46 (7): 1126 (July 1.993) reveals the calculation of geriaicidin * which is 6- (2-butyl) -3-ethyl-4-meridyl-2-manan Copper can be used as a self-regulated budding inhibitor of Strept ommycesvirid oc h-romogenes NRRL B-1551. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs

Derwent Abstract 92-166863 / 20 Unrevealed 5-iodo-6-amino-1,2-benzopiperane derivatives, optionally substituted, which are adenosine diphosphate-ribose inhibitors * treatable And prevention of AIDS-associated viruses and tumors.

Cft Selects: AID & Related l «munodef iciencies, Issue 24, 1993, Abstract 119 / 195147j Reveals the inhibitory effects of single doses of coumarin derivatives, such as favalin, 4-hydroxy-coumarin, ketosterone, For HIV-1 replication and cell-mediated or cell-free virus ____ — 17 -__-This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) No. S3100644 Patent Application Chinese Specification Correction Page (August 85) A7 V. Explanation of the invention (inhibition of f-sentence transmission. At the First National Conference on Huaan Retroviruses and Related Infections, 12-16 D ecember 1 9 9 3, Washingt ο n, D. C ., It is disclosed that coumarins, such as farwarin and piperan, such as 3- (thiophenyl) -6-phenyl-4-hydroxy-vibrone, exhibit HIV protease inhibitory effects in the analysis. The present invention proposes: "... compounds of formula I where Ri. And 1,2. Synthesis of a) Formula II or b) Formula III; where iU is -Η; where ^ is printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. A) -H * b) -OC η H 2 n + 1 * c) -F, d) -HH2- »or e) -0-C η H 2 η Η Θ t > where R 2 is a) -H ♦ b) -0 C η H 2 n + 1 * c) -cf3, d) -〇-CnH2n-CH = CH2 »or _; _- | R-This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------- --- Installation ------ Order ------- 'Λ- 线 -i /.. (Please read the cautions on the back before filling in this page) A6 B6 Staff Consumption of Central Standards Bureau, Ministry of Economic Affairs Printed by the cooperative V. Description of the invention (17) e) -0-CnHan-Het; or wherein 1 ^ and R2 synthesize a phenyl group; or wherein R0 and R2 synthesize a phenyl group; wherein IΪ3 is a) Formula IV part b) -Diphenylethyl-, c) -dibenzyl vinyl- * d) -CH- (C3-Ce cycloalkyl) 2, e) -5,6,7,8,9-tetrahydro-5H-benzene Benzeneheptenyl · f) 1,2,3,4-tetraaza-naphthyl-0 (: „1! 2» * 1, g) -CH (C „H2n * 1) -C (0) -0-C „H2„ * i * h) -CH (CH2-phenyl > 2 · i) -CvH2v-CH (R4) -CvH2v-het, or j) -CvHzv-CH (R4) -CvHzv- het-Rs; where R4 is a) b) -C Ha-C (0) * 0-C nH 2 η »1 * c) -c3-cecycloalkyl • or 'd) -C η Η 2 n ~ C 3-C β cyclofluorenyl; Where Rb is a) -Η, b) -NHa »__ c) -C (0) -CnHzn * X» d) (Zheng bit) or (meta) -0-C „H2 > t-CH = CHa, -19- (Please read the notes on the back before filling in this page) This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm) V. Description of invention (18) A6 B6 Staff of Central Bureau of Standards, Ministry of Economic Affairs Printed by Consumer Cooperatives f) g) h) i) j) k) l) m) C η H 2 nn) Het * o) p) q) r) s) t) u) v) w) x) y) -Cs alkoxy group is 0 or 1 hydroxyl group on each carbon atom. 0-C (0) -C „H2…, -Br * -CH, -Xl-CnH2n- 歯 * -Xi -CnH2 „-NH2» " Xl-CnHzn-NH-C (0) " 〇-CnH2n ^ l -Xi -C „HZ„ -CH (NH-C (0) -〇-C „Ha„ .i ) C (0) -0- »(HH-C (0) -O-CnHstMd-CniUn- -Xx-CnHzn-CH (KHa) COOH» -Xi-C „Ha„ -C (0) -0-C „HZn.x * -Xi-CnHan-Ca-Ce cycloalkyl · -CoHh-Xi -Ca-H2» -aryl, -Xl-CmHzii-0-aryl ', -Xl-CmH2m-〇-CnHan * l * -Xi-C »H2„ -C (0) -Het »-Xi-C„ HZ „-C (0) -NH-C„ H2 „-Het * -Xl -Cn Hzn ~ S-Het *- C-Hu-Xi -0-C „H2„ -Fang * · -20- This paper size applies to Chinese national standards (C NS) A4 specifications (210x297 mm) {谙 read the precautions on the back and then fill in this page}-binding. Staple. &Quot; A6 ___B6 V. Description of the invention (19) {Please read the precautions on the back before filling (This page) z) -C «Ha« -Xi-0-CnH2n-Het * al) -χ-ι * bl) -Xi-CH = CH2 * cl) -Xi-CHKH-aryl, dl) -X! -H (R4〇) 2 * el) -Xi-CnHu-Sodium imine * fl) -Xt- (pentafluoro > -phenyl, 81) -fluorene 1- "11211-bicyclo [2.2.1] Heptane, hi) -Cu-Hzu -Rao * il) -N = C- (HH-CH (C „Hz„ * 1) 2) 2 · jl) -HH-P (O) (Re) -aryl Kl) -MH-P (O) (O-Ru) -aryl "11) -HH-C (S) -HH-R42, or ml) -HH-C (S) -CH2-R4a; where: 1 is printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs a) -MH-C (0)-»b) -C (0) -HH-, c) -hh-s〇2- * d) -S〇2 -NH-, e) -HH-Soz-NH- »f) -C (0) -0- * g) -0-C (0)-, ^ h) -N (C„ H2n-aryl ) -C (0) i) -HH-C (0) -NH-, or -21- This paper size is applicable to China National Standard (CNS) A4 specification (210x297 mm) Cooperative printed A6 __ B6____ V. Description of the invention (20) j) _H [(CnH2n) e_aryl] -S 2_; where is from 0 to 5; where η is from 1 to 5; where P is from 1 to 8; where q is from 0 to 5; where r is from 1 to 8; where s is from 1 to β; where t is from 1 to 12: where u is from 2 to 6; where V is from 0 to 2; where aryl is a) benzyl is substituted by 0 to 3 㑩, b) naphthyl is substituted by 0 to 3 涸 Re, Or c) benzene is substituted by 0 to 3 Re; wherein He t is 5- or 6- and 6- or 6-unsaturated pyrene, containing 1 to 3 heteroatoms, selected from the following including nitrogen, oxygen, and sulfur; and including Any bicyclic group in which any one of the above heterocycles is fused with a benzene ring or another heterocyclic ring: and the ring may be externally linked via a carbon on the ring or a second nitrogen ring; and if chemically appropriate · ·. *! Then the nitrogen atom may be substituted by a preserving type and be substituted by 0 to 3 1s; wherein Re and R7 may be independent a) -Ci-Cs alkyl groups, substituted by 0 to 3 halogens, Or each carbon atom is 0 or 1 俚 hydroxyl substituted b) -OH · c) -Cx-Cb alkyl-OH * -22- + this paper size ^ "China National Standard (CNS) A4 specifications (210X297 (Mm) _ (Please read the precautions on the back before filling in this page) .. £ \-binding-order A6 B6 Central Standard of the Ministry of Economy Printed by the Employees' Cooperative Cooperative. V. Description of the invention (21 d) -OG-Cs alkyl, substituted by 0 to 3 halogens, or substituted by 0 or 1 hydroxy on each carbon atom, e) -〇-C2- C7 alkenyl is substituted with 0 or 1 hydroxy, f) halogen * g) -MH2, h) -NHz-Ct-CB alkyl, i) single or di-(^-"alkylamino" j) -NH- 0H, k) -M (CH2-〇H) 2 · l) -C (0) -NHZ * n) -C (0) -Ce alkyl, n) -CH0 * o) -C00H · p) -C0Xz * q) Nitro r) -CN * s) -SOaH * t) -SOaHHa · 'u) -S〇2-phenyl substituted by 0 to 3 R12 "v) -NH-S〇2-benzene Is substituted by 0 to 3 constant R12, w) -S〇2-NH-phenyl is substituted by 0 to 3 R12, X) -0 [(0Η2) 20], 0Η3 * y) -C (0 ) -0-C „H2… · z) -HH-C (O) -C« H2 „* i · -23- This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) (please first Read the notes on the back and fill in this page again)-Pack: Yes. A6 B6 V. Description of the invention (22) al) -CnH2 „-NH-C (0) -benzyl · bl) -K = N-phenyl Is 0 or 1 涸 -H (C „H2„ *: l) 2 substituted, cl) isoxazolyl, dl) pyridyl, el)-X3 ~ Cu Η 2 u-R a 〇 f 1) Fluorolinyl; Pyridyl, hi) hexahydropyridyl * 11) -MR4〇R41 * jl) -or4〇 · kl) part of formula X, or 11)-C η Η 2 B-0-C η Η 2 η ~ 0 Cn Η 2 * * 1 * where Xa is -HlUoRu; where X3 is (please read the precautions on the back before filling out this page)-binding and binding. Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs a) -〇- , B) -ciu-o- · c) -S02HR40 " * d) \ -HRaoSOz- * e) -c (0)-, f) -C (0) HR4〇- · g) n〇c (o) , Or h) -HS 4 〇-; where U is a) -Η, -24- This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) Printed by A6, Consumer Cooperatives of Central Standards Bureau, Ministry of Economic Affairs B6. Description of the invention (23) b) Phenyl, 0 to 3 涸 Re * substitution, C) -Cn H2n-Het * d) -CnHan-Ca-Ce ring sweep group * e) -Cn-Hzn ^ i » f) -Cn-H2n-CH = CHZ * g) or 2 hydroxyl groups substituted * h) -CH2-epoxidei) -C „H2„ -Ethylene oxide group * j)-(C η Η 2 η-〇) ·-C η Η 2 · ♦ 1, k) -C (0) -CeH2e ", or 1) -ch (om -ca-ce« alkyl; wherein Re is a) alkyl, or b) aryl; Where Ri i is a) -fluorene, b) -Ci-Caalkyl, c) aromatic plug, or d) its technically acceptable hydrazone »where iU 2 is a) C1-C3 fluorene * b) G-C3 alkoxy group, c) dimethylamino group, d) diethylamyl group (Please read the precautions on the back before filling this page) -25- This paper size applies to China National Standard (CNS) A4 specifications (210x297 mm) Consumption cooperation with employees of the Central Standards Bureau of the Ministry of Economic Affairs, printed by A6 B6 5. Description of the invention (24) e) CFs * f) CN, g) halogen, h) -HH2 »i) -OH * j) -C (0)-, or k) -S02-HH2-; where R30 is a) morpholinyl * b) hexahydropyridyl, c) hexahydropyridyl * d) -KR ^ oRai * e ) -OR4.0 ♦ f) part of formula X, g) -N-methyl-hexahydropyridyl, or h) halogen; wherein R4〇 and R41 are standing a) -Η or '·. · · B) -Ct-Caalkyl; where R42 is a) Ci -C4fluorenyl * or b >phenyl; the restrictions are: l) when 1 and R2 are independent -H or -0CH3 »R3 is formula IV Part, -26- This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) (Please read the precautions on the back before filling this page)-Installation, A6 B6 V. Description of the invention (25) and R4 is, then Re is not -H or -OCH3; 2) When 1 ^ is -C ^ Hh-Xi-O-Cdan-aryl, or -C »H2»- Xt-O-CnlUn-Het, then X! Is not -C (0) -HH-, -HHS〇2-, -SOz-HH- ♦ -HH-S〇2-NH- »-C (0) _0_ * -0-C (0) ~ * -NH-C (0) -NH-, -N [(C „H2„ k-aryl] -S〇2-; and 3) when IU is in part of formula IV If it is -H, then IU is a substituent containing Xi • where 乂: is -HHS〇2-; and its scientifically acceptable class. In particular * the present invention proposes compounds in which ttiO and R 2. Together they are part III. In particular, the compounds of the invention under M are proposed: compounds of formula I wherein Ri © and Rz. Synthesize Formula II; where R0 is -H; where 1 ^ is a)-Η, or b) ~ 0CnH2n + l · where 112 is ,, a)-Η, or b) -0CnHa „+ 1; where R3 is printed by the Central Standard of the Ministry of Economic Affairs and Employees' Cooperatives (please read the precautions on the back before filling in this page) a) Formula V • or b) -5,6,7,8,9-tetra-argon- 5H-benzocycloheptenyl; where R4 is -27- This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (26) a) -cyclopropyl, or b) -CmHzm * l * where Rs is a) -Η · b) -Xx-CUHa, c) -Xi-C „Ha„ -HH-C (0)- 0-C «HZn d) -Xt-C„ Ha „-CH (NH2) COOH * e > -Xi-CnHu-aryl, or f) -Xi-CmHa« -Het 5 where) is -HH-C (0)-; wherein m is from 2 to 4; wherein n is from 1 to 4 and the compound of formula I wherein R10 and R20 synthesize a moiety of formula III; wherein Ra is a) a moiety of formula V, or b)- CH- (cyclopropyl) 2; where 1U is' · · a) -C nH 2 «» .. * 1 * or b) -cyclopropyl; where IU is -H; where! ^ Is __ a) -Η »b) -C„ H2 „-CH = CH2 · (Please read the back first Note on this page, please refill this page} -28- This paper size uses tB national standard (CNS) f4 specification (210x297 mm) A6 B6 printed by A Industrial Consumer Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs 27) c) -CnH2n * l * d) _CnH; 2n-i8 propyl · e) -CH (OH > -C „H ..., or f) -CnH2n-sibrinofuranyl; where n is from 1 to 5; where pJS is from 3 to 5. The invention also elucidates: A method for inhibiting a retrovirus in a mammalian cell infected with a retrovirus, the method comprising an effective dose of M buried in the following compounds to treat the cells, the compounds include ... 4-hydroxy-3 -(or -methylbenzyl) -coumarin, 4-hydroxy-3-phenethylcoumarin, 4-hydroxy-3- (3-benzylpropyl) coumarin · 4-hydroxy-3 -Diphenylmethylcoumarin, 4-hydroxy-3- (3-hydroxy-phenylphenylbutyl) -coumarin · 4-hydroxy-3- (2-methyl-1-phenylpropyl) -Pantholin >> 4-hydroxy-3- (1-benzylbutyl) -myristotin, 4-hydroxy-3- (1-benzyl) -coumarin or coumarin, 4-hydroxy-3- (1-phenylpentyl)-· 4-hydroxy-3- (3-methyl-phenylphenyl) -coumarin, 4-hydroxy-3- (2-benzylpropyl) & coumarin, 4 -Hydroxy-3- (1,3-diphenylnoyl) -coumarin, 4-hydroxy-3- (1- (4-methylphenyl) -butyl) -coumarin, coumarin Element, 4-hydroxy-3- [l- (4-hydroxyphenyl) propyl] _ · -29- This paper uses the national standard (CNS) A4 specification (210X297 mm) (Please read first Note on the back * Fill in this page again} -Installation ". A6 B6 V. Description of the invention 28) 4-Hydroxy-3- (1- (1-naphthyl) -propyl) -myristotin · coumarin, 4-hydroxy-7-methoxy-3- (1-phenylpropyl)- · Coumarin · 4-hydroxy-6-methoxy-3-U-phenylpropyl)-, coumarin, 4,7-dihydroxy-3- (1-phenylpropyl)-* coumarin * 4,6-dihydroxy-3- (1-phenylpropyl)-, coumarin, 4-hydroxy-7-methyl-3- (1-phenylpropyl >-coumarin, 7- Chloro-4-hydroxy-3-U-phenylpropyl >-»coumarin, 4-hydroxy-3- [l- (4-methoxyphenyl) propyl] myristotin * 4-hydroxy-3 -[l- (3-hydroxyphenyl) propyl]-* 4-hydroxy-3-U-phenyl-2-propenyl) -myristotin * myristotin * 3-U-ethyl-para-position -Fluorobenzyl) -4-hydroxy- * 4-hydroxy-3- [l- (l, 2,3,4-tetraaza) -naphthyl] -myristole, 4-hydroxy-3- [l- Hydroindenyl] -coumarin * and 4-hydroxy-3- (1-phenylpropyl) -coumarin. In addition, the present invention proposes a compound of the formula M: a compound of formula V 11 wherein R 4 is a) C »Η 2 · + 1, or, b) cyclopropyl; wherein 1 {5 is a) -Xx aryl, Ministry of Economic Affairs Printed by the Central Bureau of Specimen Shellfish Consumer Cooperatives b) _Xi-CmHa * ~ Het * c) -Xi-CHKH-aryl, d) -Xx-C „H2„ -HH-C (0) -〇-C „ H2n * i * -30- This paper ― Ι / Οΰί uses Fa national standard (Clis) A4 specification (210 X 297 mm) (Please read the precautions on the back before filling this page) Printed by the Industrial and Consumer Cooperatives · A6 B6 V. Invention Description (29) e) -Xi-C «H2i:» i · f) -Xi-C.H2.-CH (KH-C (0) -O-CBHzn ^ tiCnHa »-Het, or. g) -Xx-CnH2» -®; where Xi. a) -MHSOa- * or b) -HHC (0)-; where "is from 0 to 4; where n is from 1 to 4; where P is 3 or 4 · · where t is 3 or 4; where aryl is a) phenyl is 0 to 2 Re substituted * or b >phenyl; where Het is 5- or 6-membered saturated or Unsaturated fluorene contains heteroatoms selected from 1 to 3, including: fluorene, oxygen, and fluorene, and includes any bicyclic group, in which any of the above heterocycles is fused with phenylhydrazone or another heterocycle; and 〇 to 2 R ? Substituted; and pharmaceutically acceptable salts thereof. In particular, the present invention proposes such compounds: wherein the aryl group is phenyl; where Het. Is __ a) imidazolyl * b) quinolinyl, -31 -This paper size is in China B Standard (CNS) A4 size (210X297mm) ............. Mark ... ............... d · (Please read the notes on the back before filling this page)

A6 __B6 V. Description of the invention (30) c) Benzothiadiazolyl * d) Benzofuryl, e) Thiophenyl, or f) pyridyl; where Re is a) methyl · b) ethyl · C) -Cl, d) -P, e) -Br »f) -I · g) -H〇2 · h) -0CH3, i) -CFa * j) -CN · k) -C00H * 1) -N = N-phenyl, m) -NH-0H · n) -H (CH3) * * o) -NHz * P) -0CF3, q) -CHa-Br * r) -C (0) HH2 · s) -C (0) 0CH3, printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs {Please read the precautions on the back before filling this page) -32- This paper standard uses China National Standard for Standards (CNS) A4 (210X297mm) V. Description of the invention (31) t) -OH * u) Formula X part · V) -CH2〇H, w) -HH- (CHa) 3-0H · x) -H ((CH2 ) 2-0H> 2, or y) -MHS〇a- (CH2) 3-C1; where R7 is a) methyl · b) -s〇2-phenyl, c) -Cl, d) -Br * e) isoxazolyl, or f) yang: pyridyl; where 1 {8 is -H; A6 B6 (please read the precautions on the back before filling this page). Binding ... Staff of Central Bureau of Standards, Ministry of Economic Affairs Printed by consumer cooperatives where u is 3. More specifically, the present invention proposes a compound of the following formula: a compound of formula V 111 wherein R4 is ''! B) cyclopropyl; wherein Rs is a) -Xi-aryl, __ b)-Xα-Het * or c)- Xi-CH (NH-C (0) -0-C »H2„ * i) -CH2-Het; 4--. -33- The standard of this paper is the national standard (CNS) A4 (210X297) (Mm) Printed by A6 B6, Shellfish Consumer Cooperative of the Central Sample Bureau of the Ministry of Economic Affairs 5. Description of Invention (32) where Xi is a) -NHS〇2- • or b) -HHC (O)-; where m is from 2 To 4; where η is 4; where aryl is phenyl which is substituted by 11! 1 «; where Het is 5- or 6-beam and or not, and contains a ring * containing from 1 to 3 Fluorene atom, including nitrogen, oxygen, and hydrogen, and including any bicyclic group, any one of the above fluorene rings may be fused with a benzene ring or another fluorene ring; and is substituted by 0 or 1 R? And its pharmacy Acceptable salts. More particularly • The present invention proposes compounds under K: compounds of formula IX where Rs is a) -NHS〇2-aryl • or b) -MHSOz-Het; where aryl is phenyl is 1 Replaced by a R *; where Het is 5- or 6-Beacon and into a planer and ring * contains from 1 to 3 Burmese from the following Atoms include fluorene, oxygen, and sulfur, and include any bicyclic group, in which any of the above heterofluorenes can be fused with a benzene ring; and substituted with 0 or 1; and its pharmaceutically acceptable salt f »especially The present invention proposes such a compound: where Het is -34- This paper size uses the Chinese National Standard (CNS) f4 (210x29.7 mm) (Please read the precautions on the back before filling in this page}. Binding. A6 __B6__ 5. Description of the invention (33) a) quinolinyl · b) benzothiadiazolyl · or c) oxazolyl; where Re is a) -CH · b) -Cl »c) -F * d) -MHOH * e) -C (0), f) -C (O) OCHa · g) Formula X, h) -HHS〇a- (CHZ) 3-C1 »X) -CH2 -0H * or j) -N ((CH2) z-0H) 2; wherein R7 is methyl; wherein u is 3; and pharmaceutically acceptable salts thereof. Meanwhile, the present invention proposes: ~

, ... I A method of inhibiting a retrovirus in mammalian cells infected with a retrovirus, the method comprising administering to the cell an effective dose of a compound of formula I (Please read the precautions on the back before filling in this page) Among them Ri. And R20 synthesis__ a) Formula II, or b) Formula III; -35- This paper size adopts China National Standard (CNS) A4 specification (210X297 mm). Printed by the consumer cooperative A6 __B6_ V. Description of the invention (34) where R0 is -H; where 1 is a) -Η * b) -0CnH2nfl * c)-F »d) -hh2-» or e)-0- Cn Ha η _ H et ί where R2 is a)-H »b) -OC.nHan-1 * c) -CP3, d) -O-CUHKIU, or e)-0-Cn H a η _ H et ί Or wherein 1 ^ and R2 synthesize phenyl, or R0 and R2 synthesize phenyl; wherein R3 is a) a moiety of formula IV, b) -diphenylethylfluorene, '.--c) -distyryl -· D) -CH- (C3-Cecycloalkyl) 2 »e) -5,6,7,8,9-tetrahydro-5H-benzylcycloheptenyl, f) -1,2,3 , 4-tetrahydro-Zeiki-0 (: „112„ .1, g) -CH (CnH2n * l) -C (0) -〇-C „H2n.l * h) -CH (CH2-phenyl ) 2 · -36- This paper size adopts China National Standard (CNS) A4 specification (210X297mm) ............... .............. r ............ ........................... TΓ .............. ....... line {please read first (Read the notes on the back and fill out this page)

Printed by A6 _B6_ of the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs V. Invention Description (35) i) -CvH2v-CH (IU) -CvH2v-het, or j) -Cv Hz v -CΗ (R 4) -C vH av-h e tR s; where R4 is 3) —CmHae * l * b) -CH2-G (0) -0-C „H2„ * i · c) -Cs-Ce cycloalkyl, or. d) -{^ "《-(^-{^ Cycloalkyl; where" is a)-Η »b -KHa» c) -C (0) -C „H2„ * i · d (adjacent) or (between Position) -0-C „H2„ -CH = CH2, e -Ca-Cs alkoxy group, substituted with 0 or 1 Burmese hydroxyl group at each carbon atom, f -〇-C (0) -CnH2n- »l * g -Br »h) -CH, n -C.Ha.-Xt-CtHii: *!. '· j / -Xl_CnH2« _ by, k) -Xx-CnHzn-MHz · Π -Xi-C „H2n -MH-C (0) -0-C „H2„ * ia -Xi-C „H2« -CH (HH-C (0) -0-C „H2„ * 1) C (0) -0-C »H 2 n» 1 'n) -Xi-C-lUm-CiUNH-nin-O-UIUn + O-CniUn- -37- This paper standard complies with ti £ .3 home standard (CNS) A4 specification ( 210X297mm) {Please read the precautions on the back before filling this page) -Installation, ej. .-Refer to A6 B6 V. Invention Description (36) Het * 0) -Xi-C „H2» -CH (HH2) C00H »p) -Xi -Cn Hzn ~ C (0) -0-C nB 2n ♦ 1 * q) -Xl " Cn H2n & qu ot; C3 -Ce cyclofluorenyl * r) -C »H2» -Xx-C. -Hh-aryl * s) -Xl ~ C «H2m * ~ 〇-aryl / t) -X1-C» H 2-0-CnHen + 1 * (Please read the notes on the back of the fund before filling out this page) Central Standards Bureau of the Ministry of Economic Affairs, Bei Gong Xiao #Cooperative Society Printing u) -C «H2-X1 -C * Ha-Het * v ) -Xi-C „H2n-C (0) -Het» w) -Xi-C „HZ„ -C (0) -HH-C „H2n-Het * x) -Xi-C„ H2 „-S- Het · y) -0-CnH2 „-aryl, Z) -CmH2 ·-Xl ~ 0-CnHzn-Het * al) -Xi-H» bl) -Xi-CH = CH2 · cl) -Xi-CI ^ CH-aryl, d 1) _ X 1-K (R 4 O> 2! * El) -XrCnHh-phthaliminoimine, 'Can-fl) -Xi- (pentafluoro) -phenyl, 81) -fluorene 1-(: „112„ -Bicyclo [2.2.1] heptane, hi) -Cu-Hau'Rao * il) -H = * C- (NH-CH (C „H? N ^ i) a) a ^ jl) -HH-P (O) (Re) -aryl group, kl) -NH-P (O) (0-U-aryl group. · Binding. Binding. -38 " This note XS is suitable for China country (Take TCNS) A4 specifications (210X297 male f) A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (37) 11) -NH-C (S) -NH-! U2 ) -NH-C (S) -CH2-IUa; where Xi. A) -NH * ~ C (0)-, b) -C (0) -HH- · c) -NH-S〇2-, d ) -S〇2-NH-, e) f) -C (0) -0- * g) -0-C (0)-* h) -K (C „H2„ -aryl) -C (0)-, i) -NH-C (0 ) -HH-, or j) -N [(C »H2« > aryl] -S〇2- where B is from 0 to 5; where n is from 1 to 5; where P is from 1 to 8; Where q is from 0 to 5; where Γ is from 1 to 8; 'where s is from 1 to 6; where t is from 1 to 12 ί where u is from 2 to 6; where V is from 0 to 2;- Wherein aryl is a) phenyl is substituted by 0 to 3 Re -39- This paper size is based on China National Standard (CNS) A4 specification (210X297 mm) ........... .............................. ir ... ..................... TΓ ...... ............. Wire (please read the precautions on the back before filling this page) 5. Description of the invention (38) b) Naphthyl is 0 to c) Foot phenyl is 0 where Het It is 5- or 逦 from the following heteroatom ring groups: where any of the above can be bonded via a carbon or a ring on the ring. Then the nitrogen can be a nitrogen atom in which Re and R7 are each a) -Ci, 0 or 1 on hydroxyl on Ce 焼 b) -OH · C) _Ci_Cs 焼 6-Basket 3 «Re replaced by 3 俚 Re take saturated or Insaturation includes: • Nitrogen, oxo may be combined with phenylhydrazone, or the out-of-ring atom may be lithium argon A6 B6, or substituted for $ and 瓌 • contains from 1 to 3 «and 礞 • and includes any two or other A heterocyclic ring is fused; and a ring nitrogen is connected; and if it is a chemically modified plastic formula; if it is chemically protected by a protective form; and is substituted by 0 to 3 俚 117; Or replaced by the original carbon base, radical -0H, printed by the R Industrial and Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs d) -O-Ci-C〗 Alkyl is replaced by 0 to 3 teeth, or on each carbon atom Substituted with 0 or 1 hydroxy, e) -0-C2-C7 alkenyl, substituted with 0 or 1 hydroxy, 0 halogen, g) -NHz * h) -Nh-Cii-Cs alkyl, i)箪 mono- or di-(^-(^ alkylamino, j) -HH-0H, k) -H (CHz-OB) 2 _ l) -C (0) -HH® »a) alkyl * 40 Paper Size Uses National Standard (CNS) A4 Specification (210x297mm) .................... .........: κ.: ί ...... install ............. Tr .............. i cable (Please read the precautions on the back before (Fill in this page) A6 __B6 _ V. Invention (39) n) -CHO · 〇) -C00H * P) -COX2, q) nitro · r) -CH »s) -SOaH * t) -SOaHHz · u) -S0 2-phenyl is 0 to V) -NH-S〇2-phenyl is substituted by 0 to 3 Ria -S02-MH-benzyl is substituted by 0 to 3 R12-X) -0 [( CHa) 20], CH3 * y) -C (0) -0-C „H3… · z) -HH-C (0) -C„ Han * i · al) -C „H2„ -HH-C ( 0) -phenyl * bl) -M = H-phenyl * is 0 or 1 substituted * cl) isopidazolyl * dl) pyridyl, el) ~ Xa-CuΗ2u ~ R »〇 * fl) _ 祢Porphyrin: gl) hexahydropyridyl * hi) hexahydropyridyl * Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the notes on the back before filling this page) il) ~ HR «〇R4i * _ jl) -or4〇 · kl) Part of Formula X, or -41- This paper size uses China National Standard (CNS) A4 specifications (210x297 mm) A6 B6 5. Description of the invention (4〇) Ministry of Economy Printed by the Consumer Standards Cooperative of the Central Bureau of Standards 11) " Cnfl2n " 0 ^ C * iH2n " 0CnH2fi * l * where XaS -NIUoRo; where X3 is a) -〇- * b) -CHa * c) " SOzMRaO " * d) -MR ^ oSOa * * e) -C (0)-* f) -C (0) NIU〇-, 8) -NR4〇 C (0), or h) * NR 4 〇 * * where Re is a) -H · b) -C "HZn-phenyl is 0 to 3 substituted by Re c) -CnHzn-Het * d) -C „H2„ -C3-Ce cycloalkyl, e) f) -C „H2„ -CH = CHa · ", < g) is substituted by 1 or 2 hydroxyl groups h) -CH2-epoxide * i ) -C „Ha„ -Ethylene oxide, j) _ (CnH2B " * 〇Hn-CnJa.n * l * k) -C (0), or 1) -CH (0H) -C3-Ce ring Alkyl; -42 * (Please read the precautions on the back before filling this page) This paper size uses China National Standard (CNS) A4 specification (210X297 mm) A6 B6 Employees of the Central Standards Bureau of the Ministry of Economic Affairs # Printed by the cooperative V. Description of the invention (41) where "is a) -Ci-C · * sulfonyl * or b) aryl; where Rn is a) -Η · b) -CrC ^ i alkyl plug" c) aromatic D) its scientifically acceptable salts; where R12 is a) Ct-c3 ^ m · b) Ci-C »alkane, c) dimethylamino * d) diethylamino, e) CF3, f) CN · g) by, h) -HH2, i) -OH · j) -C (0)-· or k) -SOa-MHa-; where Rs0 is a) B) Hexapyridyl; c) Hexahydropyridyl ... . .................. K .............. i .... ......... ΤΓ .......... Λ. {Please read the notes on the back first (Fill in this page again)

-43- The paper size is in accordance with China National Standards (CNS) Sub 4 Specification (210X297 mm) A6 _B6_ V. Description of the Invention (42) d) _NR4〇R41 * e) -OR · *. , F > part of formula X * g) -fluorene-methyl-hexahydropyridyl • or h) halogen: where R · *. And R41 are independently buried from a)-fluorene or b) alkyl; wherein R42 is a) CU- "alkyl, or b) phenyl; the restrictions are: 1) when 1 ^ and R2 are -H or- -〇CH3 · R3 is a moiety of formula IV and IU is -C-Hw: 1, Lang Rs is not -H or -OCH3; 2) When Rs is aryl or -C ^ Hh-XrO-CxIUn-Het, X! Yes -C (0) -MH-, -NHS〇a- • -SOa-NH- · -HH-S〇a-HH-, -C (0) -0- * -0-C (0)-· -HH-C (0 > -NH-, -N (:( CnH2n) '> aryl] -S〇2-; and 3) when R4 is -H in the part of formula IV, then Rs contains Substituents of ^ * where ^ is -HHS〇2-; and its scientifically acceptable salts. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling the nesting page). Finally * The present invention proposes: __ A method for preparing a compound of formula XI * This method includes: -44- This paper size uses the Chinese National Standard (CNS) A4 specification (210X297 mm) Ministry of Economic Affairs + Sample Standards Bureau Shellfish Consumer Cooperative Printing A6 ____B6__ V. Description of the invention (43) a) Compound of formula XII and compound of formula XIII • Performed in a hydrocarbon solution and in a high temperature in the presence of a trialkylamine, which can generate a compound of formula XIV B) treatment of the compound of formula XIV in water / fermentation mixture: and c) treatment of K acid b) step lavage • can generate formula XI containing compounds. The compounds of the present invention are named after IUPAC or CAS. Suspended carbon atoms of various sulfo-containing parts * are indicated by the prefix. • The minimum and maximum numbers of sulfonic atoms in the part are indicated, that is, the prefix C ^ -Cj represents the integer "i" to the integer "j" Part of an atom, and includes two. Therefore • For example, Ct-Ca alkyl pseudo refers to an alkyl group with 1 to 3 fi carbon atoms. Or methyl, ethyl, propyl, and propyl, straight and branched versions. At the same time • The carbon atom content of various hydrocarbon-containing parts of the present invention * is represented by an integer written below, representing the number of carbon and «atoms * in the part * such as" C „h2n" means "n" and the number of carbon atoms ( Including this number) and the "2n" integer number of argon atoms (including this number). So * like "CBH2n" where η is from 1 to 3 carbon atoms, and from 2 to 6 argon atoms, or methyl, ethyl, propyl, and isopropyl * and all of its isomers, straight, and branches Style. Examples of alkyl groups from 1 to 9 carbon atoms are methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, 'octyl and nonyl, and all their isomers ... Type and its straight and branch style. Examples of alkenyl groups from 1 to 5 sulfonic atoms are: vinyl, propenyl, butenyl, pentenyl, all their isomeric forms and their straight or branched forms. "Halogen" means a typical halogen atom, such as Dai, chlorine, bromine and iodine. The compounds of formula I according to the invention can inhibit the retroviral protein * and therefore can inhibit virus replication. It can be used to treat the infection of human immunodeficiency virus (please read the precautions on the back before filling this page) -45-This rule of skin speed is applicable to national standards (CNST? 4 specifications (210X297) «) Ministry of Economic Affairs Sample A6 B6 printed by the quasi-quasi bureau Shellfish Consumer Cooperative 5. Patients of Invention Note (44) (HIV) • This virus causes acquired immune deficiency microclimate (AIDS) and related diseases. More specifically, the compounds of the present invention can Acts as a novel inhibitor of human retroviral protein. Therefore, * compounds can inhibit retroviral protease and thus inhibit disease replication. It can be used to treat human patients infected with human retrovirus, such as human immunodeficiency virus ( HIV-ι or HIV-2 strains) or human T-cell leukemia virus (HTLV-I or HTLV-m), which causes acquired immune deficiency stress groups (AIDS) and / or phase-out diseases. Retroviruses are protein-like and replicated Enzymes (ie, proteases, reverse transcriptases, and plums) are translated from the gag and pol genes of the virus · M polyproteins • Types are further modified for viral protease (PR) processing to become heat proteins 为 for viral function and replication In the case of essential viral proteins, prions cannot replicate if PR is absent or non-functional. Retroviral PR, such as HIV-1 PR, is an asparagine prion protein _ * its active position characteristics Similar to that exhibited by the more complex aspartate protease-enzyme. Regulated human reverse transcriptase (HRV) includes human immunodeficiency disease type I, human immunodeficiency patient type, or its # 糸 * Μ and human T-cell leukemia viruses 1 and 2 (HTLV-1 and HTLV-2), or products seen by spermologists · They belong to the same or related virus family, which can cause similarity in humans as various human retroviruses The physiological effects of patients should be treated as follows: 1) those infected with a human retroviral strain of M * are determined by the presence of detectable virus antibodies or antigens in M serum, and in HIV cases * Symptoms of HIV infection or symptoms -46-This paper size uses the Chinese National Standard (CNS) A4 specification (210X297 mm) {explain the precautions on the back before filling out this page}-binding Α6 Β6 Ministry of Economy Printed by the Central Standards Bureau Shellfish Consumer Cooperative Explanation (45) A IDS clear infection • such as i) Lan diffuse sister is suspected of plasmomycosis · fi > Psoriasis xingensis · bronchopulmonary and candidiasis of the lung, including pulmonary sac pneumonia, iv > Lymphatic ridges, or V) Kaposi's sarcoma, and under 60 years of age K; or CD45 lymphatic ridges in blood surrounding it are less than 500 / mm 3. Treatment includes maintaining a level of inhibition of the compound of the present invention in the patient for a period of time * and continuing until the second symptom, AIDS, which clearly indicates the need for additional therapy, develops a clear infection. More specifically * An example of such a human retrovirus is the human immunodeficiency virus (HIV, also known as HTLV-B or LAV) * It has been masculine as one of the human acquired immune deficiency syndrome (AIDS) Pathogens · P. Duesberg, proc. Hatl. Acad. Sci. USA, 86: 755 (1989) (HIV contains a protease encoded by a retrovirus. HIV-I protein plum. It can lyse fusion peptides into Functional proteins of thermoviral particles · EP Lillehoj, et al., J. Virology, 62: 3053 (1988); C. Debuck, et al., Proc. Hatl. Acad.

Sci., 84: 8903 (1987). This enzyme * HIV-1 protease has been classified as aspartate-like protease and has proven homogeneity with other aspartate-like proteins (such as renal enzymes) * LH Pearl, et al., Nature 329: 351 (1987); I. Katoh, et al., Mature 329: 654 (1987) The inhibitory effect of protein -1 can block the replication of HIV * and can therefore be used for Treatment of AIDS in humans, ED Clerq, J. Med. Che ·. 29: 1561 (_1986 > «HIV-1 protease inhibitors can be used to treat ringworm Η IV infections * It is a symptomatic or asymptomatic AIDS patient.

-47- This paper uses China National Standard (CNS) A4 specifications (210X297 mm) < Read the notes on the back before filling in this page > • Binding. Staff Consumer Cooperatives, Central Bureau of Standards, Ministry of Economic Affairs Print A6 _; _B6_ V. Description of the Invention (46), Pepsin A • is a general inhibitor of aspartame, and has been shown to be an inhibitor of HIV-1 protease * S. Seelaeier, et al., Proc. Hatl. Acad. Sci. USA. 85: 6612 (1986). Other substrate-derived inhibitors containing buried primary bond isotopes or inhibins at breakable sites are also shown, ML Moore, et al., Biochem. Biophys, Res. Consun. 159: 420 (1989); S Billich, et al., J. Biol. Che .. 263: 17905 (1988); Sandoz, DE 3812-576-A. Therefore, the compounds of the present invention can be used to treat diseases caused by retrospective diseases * such as humans. Houyi immune deficient micro-climate (AIDS). Compounds can also be used to treat non-human animals infected with retroviruses, such as cats with feline leukemia virus. Other feline infectious viruses include: feline infectious enteritis Virus, calicivirus, rabies virus, feline immunodeficiency virus, feline ribosuccinic acid disease (granulocytosis virus), and feline chlamydia. Exact dose of the compound of the present invention for non-human animals * The pattern and chess pattern should be obvious to ordinary artisans, such as veterinarians. The compounds of formula I of the present invention can be prepared as described in the procedures, preparations and examples below, or can be prepared by similar methods.榇 Synthesis, technical «person is easy And applicable. The procedure A is based on the literature method (R. B. S i 1 vers η a η, J. A m. Wolff, KP Lin.k, J. Am. Chem Soc. 65: 2285-2287 · 1943) · Acidation mediated by diisopropylcarbodiimide and catalysis by dimethylaminopyridine -48-Ben Paper size: National Standard (CNS) A4 specification (210X297 mm) < Please read the note on the back first 苒 Fill the page}-Binding-Book A6 _ B6 _ V. Description of the invention (47) Ethyl salicylate of the formula A-1 is the effect of stilbene carboxylic acid, especially 4-phenylbutanoic acid and 5-phenylvaleric acid, which can provide substrates of the formula A-2 and A-4, respectively. Sodium hydride is treated in refluxing benzene to achieve ring closure on substituted 4-hydroxycoumarins of formula A-3 and formula A-5. Process B is based on literature methods. (G. Appendi η 〇, G. C rav 〇11 〇, S.

Tag 1 iapietra, S. Ferraro, GM Nano, G. Palnisano, HCA 74: 1451-1458, 1991), M-type B-2, Xue-treated formula Bl, commercialized 4-hydroxymyristotin, where R is naphthalene- 2-yl, diphenylmethyl, or α-methylbenzyl (prepared according to Scheme C) Structure, wherein R is naphthyl-2-yl • benzyl, or α-methylbenzyl. The yield of this reaction is highly variable, possibly due to the different solubility of the product, which can be roughly separated by filtration in the autoreaction mixture. Sodium cyanoborohydride can complete the primorogenic lysis of dimer B-3 in refluxing methanol to produce compounds of formula B-4a, B-4b or B-4c. Similarly, yields and reaction times can be highly variable. In response to MUC tracking, it may be necessary to add another portion of sodium fluoroborohydride for a period of time. , Process C The preparation of the aldehydes of formulas C-3 and C-6 commonly required in the process B is explained in Process C. 2-Naphthaldehyde is commercially available. Commercial carboxylic acids of formulas C-1 and C-4 can be derivatized into their methyl (M-methoxy) fluorenamines, using bis (2-oxy-3-oxazolyl) phosphine chloride as the coupler . Μ lithium aluminum hydride in the 2: chain through the original (JA, Fehrentz, B, Castro, Synthesis. 676-678, 1983) Keping-49- _ This paper standard uses the Chinese national standard (CNS) f 4 Specifications (210x297 mm) {Please read the notes on the back before filling this page}.

Printed by the Order of the Ministry of Economic Affairs, Bureau of Standardization, Shellfish Consumer Cooperatives. 5. The invention is clear (48). Steady production of D stream. Alkylation into Titus, 1957; Trager M D-2. Formula 4-hydroxyl. In this way, the aldehydes of formulas C-3 and C-6 are formed by benzene benzene A6 and B6. Process D describes 4-hydroxymyristotin used directly at various temperatures with various benzyl aluminas. This is based on literature methods (CH Schroeder, EDKP Link, J. Ab. Chea. Soc. 79: 3291, LR Pohl, R. Haddock, WA Garland, VF, J. Med. Che. 18: 513, 1975). U-bromoethyl > benzene (where R is α-methylbenzyl) of formula M under 155υ treatment of product D-1 4-hydroxymyristotin, which can produce 3- (cc -methylbenzyl) coumarin (where R is α-methylbenzyl) The method can also be used to prepare additional compounds, including 4-hydroxy-3- (2-methylpropyl) _myristole And 4-hydroxy-3- (1,3-dibenzylpropyl) -myristole (Formula 3, wherein R is 2-methyl-phenylphenylpropyl or 1,3-diphenylpropyl). Straight group. D wave 4-hydroxy Gar i an AC alkylation seems to be limited by holding the base which plays a more intense reaction ............... ................................................... ....... Installation ............ < 谙 Read the precautions on the back before filling in this page} Ministry of Economy The printing process of the Consumer Standards Cooperative of the Central Bureau of Standards is also described in accordance with the literature procedure * Adhesion of substituents to the 3-position of myostatin using benzylase (L.8. Polh, R. Haddock, WA d, VF Trager, J.Med Che .. 18 ^ 513, 1975; n, A. Kuaar, PC Ray, Indian J. Che .. 25B: 6 ^ 3, 1986). The reaction is quantified by Lewis acid, and boron trifluoride etherate should usually be removed. 3- (Cyclopropylphenylmethyl) -4-hydroxycoumarin of formula D-3 (wherein R is cyclopropylbenzylmethyl) is prepared from the α-ring of formula D-4 in a yield of 50¾. Propyl glutamate (wherein R is cyclopropylphenylmethyl) and 4-hydroxymyristotin of formula D-5 in the presence of dioxane and a large amount of trigas boron ether «50_ This paper size Applicable to China National Standard (CNS) A4 specification (210X297mm) A6 B6 5. Description of invention (49) The office of the director and the middle of Shanghai responded overnight. The main by-products appear to be derived from the benzylic elimination that starts under the reaction conditions. Most of the compounds of the present invention can be prepared by this method. ε scheme 3-1 Ethyl benzylhydrazone and methylphosphonic acid dimethyl ammonium tert-butoxycarbonyl glycemic male and female, using MH2 / benzene reaction to form E-2 unsaturated sugar, showing E RZ isomer mixture. This diastereoisomeric mixture is catalyzed by Pd / C. Hydrogenation in ethyl acetate * yields a saturated compound of formula E-3. Nitrile functionality followed by KM potassium oxide hydrolysis • Utilization of water-acetic acid "can generate equivalent acids such as compounds of formula E-4. The acidic functional group in free state utilizes isobutylene and acid to catalyze dioxane to protect the third butyl ester protecting group of the compound of formula E-5. The enolytic acid of the compound of the formula E-5 formed by the treatment with lithium dioxopropyl-amine lithium is reacted with the methyl hydrochloride to form a Claisen condensation product of the formula E-6. Treatment with trifluorophosphonic acid can achieve the hydrolysis of the protective group of the third butyl ester, and also results in the closed-loop product of the formula E-7. The acid of the formula E-7 can be condensed with various amines, such as the third butyl glycine Esters * use diethylcyanophosphonate as myronate to form equivalent endamines such as 4-hydroxy-3- (1- (3-((((1,1-dimethyl Ethoxycarbonyl) methyl) amino) carbonyl) phenyl) ethyl coumarin). F Printed by the Ministry of Process Economics, T.L.S.Beige Consumer Cooperative (please read the precautions on the back before filling this page) meta-nitroethyl benzyl ketone and methylphosphonic acid dimethyl tert-butyl The danger of oxycarbonyl esters is the use of sodium hydride / benzene reaction to produce unsaturated vinegar of formula F-2, which is a mixture of E and Z isomers. This diastereomeric 髑 异 # mix-51-^ # i ? (CNS) > 7 ^ «T21〇x297 ^ at) ii51 · "-Printed by A6 _____ B6_ of the Consumer Cooperatives of the Ministry of Economic Affairs + Central Sample Standard Bureau V. Invention Description (5〇), using Pt / C as The hydrogenation of the catalyst (50 psi hydrogen, formic acid) produces a saturated amine compound equivalent to formula P-3. Free-state amine functional groups, protected with tris-tris-methane and diisopropyl-z-amine treatment, can form tris-methyl compounds of formula F-4. The enolic acid of formula F-4 (formed by treatment with diisopropylglycosamine) reacts with salicylic acid to form a Claisen kneaded product of formula F-5. K trifluorosaccharic acid treatment can achieve the hydrolysis of tertiary butyl alcohol and the hydrolysis of tribenzylmethyl * protecting group. It also results in the closed-loop product of formula F-6. An amine of formula Fq can be condensed with various carboxylic acids, such as Boc- / 3-alanine, and diethyl cyanophosphonate is used as a mixture agent to generate a comparable end product of recommended amine (eg, 4-hydroxy-3- (1 -(3-((3-((1, Dimethylethoxycarbonyl) amino) -dioxopropyl) amino) phenyl) propyl pumycin. Next M trifluoric acid Treatment can generate equivalent free-state amines (eg, 3-U- (3-((3-amino-1-oxypropyl) amino> phenyl) propyl) 4-hydroxy-coumarin * Trifluoroacetate). G Laicheng adds ethylmagnesium bromide to 3-hydroxybenzaldehyde to produce a compound of formula G-2, which can be alkylated with allyl bromide to produce a compound of formula G-3. 4 -Hydroxy melamine and the compound of formula G-3 and the use of trisated sulfonium etherate as an acid-catalyzed surface reaction can generate a compound of formula G-4 (such as 3- (1 '-(3-allyloxy Phenyl) propyl) -4-hydroxymyristotin). Compounds of formula G-4 can be dihydroxylated with osmium tetroxide to produce compounds of formula G-5 (3- (1 ·-(3-((2, 3-Diphenyl) propoxy) phenyl) propyl) -4-hydroxymyristotin). Ηprocess-52- This paper size applies to China 21_ 家 搮 准 (CNS) 甲 4 Grid (210x297 mm (please read the precautions on the back first, and then go to the next page). Binding Book No. 83100644 Patent Application Chinese Manual Correction Page (August 85) A7-B7 V. Description of Invention (X /) Economy The Ministry of Central Standards Bureau ’s Consumer Cooperative printed the formula H-1 of 1- (4-Cyclophenyl) with acetic anhydride in pyridine to produce a compound of formula Η-2, which was reacted with 4-hydroxycoumarin Shaved salt reaction can produce a compound of formula Η-3, ρ- (ΐ,-(4-ethoxyfluorenylphenyl) propyl) -4-hydroxycoumarin). I 3-phenyl of formula 1-1 The reaction of 2-propyne-butanol with 4-hydroxycoumarin in the presence of diethyl azobisacid vinegar and triphenylphosphine can generate a compound of formula 2 with M hydrogen and Lincnar :, S > The catalyst part is original, which can generate compounds of formula 1-3. The compound of formula BU 3 in phosphine xylene can be heated at 145 to produce the compound of formula 1-4 (4-hydroxyl-3- (1- Phenyl-2-propenyl) -coumarin). Process J Preparation of the compound of formula J-3 of the present invention (where Ri is ethyl, R2 is phenyl * is cyclopropyl, R2 is phenyl; 1U is ring Propyl, r2 is cyclopropyl; Cyclopropyl, h is meta- (nhco2-benzyl) phenyl; is benzyl * 1 is benzyl; where η is 4) from known piperanone intermediates of formula J-1 (where η is 4 ) And the secondary fermentation of J-2 (where 1 ^ and 1? 2 are as shown in formula J-3), alkylated in the presence of para-toluenesulfonic acid, as shown in the J scheme. Piperanone (where η is 4) is prepared by the fermentation of trimethylsilylenzyme and malondichloride, such as R. Effenberger, T. Ziegler, K.-H. Schonwalder, T. Kesmarszky , B. Bauer, Chem. Ber. 119: 3394-3404 (1986). Alcohols of formula J-2 (where h is ethyl * R 2 is phenyl; R ·! Cyclopropyl * R 2 is phenyl; Ri and R 2 are each cyclopropyl) are commercially available. Fermentation of formula J-2 (where 1U is cyclopropyl and h is ._____ " _5 ^ _ 二 _——--------- This paper size applies to China National Standard (CNS) A4 (210X297 mm) ) (Please read the note on the back # ^ fill in this page first)-Binding. Thread No. 83100644 Patent Application No. Printed Chinese Manual Correction Sheet (August 85) printed by the Chinese Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Description of the invention Meta- (NHC02 benzyl) phenyl; and r2 are each benzyl) were prepared as described in the preparation method below. In most examples, the excess alcohol M is used for alkylation, and water The K can be refluxed from the reaction mixture through a molecular sieve column, or removed by adding a sieve to the reaction mixture. In several examples, 3- (dicyclopropylmethyl) -5,6, 7,8, 9, 10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperan-2-嗣 and Aminocarboxylic acid, [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl]-, benzyl methyl ester, reaction conditions changed slightly. In 3- (diphosphoniummethyl) -5,6,7,8, 9, 1 0 -hexahydro- 4-hydroxy-2H-cyclooctyl [b] nanan-2- 嗣 (η is 4 ^ Ri And R 2 is cyclopropyl) because the product is unstable under the reaction conditions, a shorter reaction time is used. [3-] cyclopropyl (5,6,7,8,9,10-hexahydro-4 -hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) In the example of methyl] phenyl] -phenylmethyl ester (η is 4, 1U is cyclopropyl * R2 is meta- (NHC〇2benzyl) phenyl), because alcohol is not commercially available, it is used Slightly larger amount of pipera. The K scheme is as described in the K scheme. * Amidyl formic acid * [3- [Cyclopropyl (5,6,7,8 t 9, 10-hexahydro- 4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-* phenylmethyl ester (benzyloxycarbonyl protecting group on formula K-1) can be easily catalyzed by the hydrogenation of hydrocarbons in solvents such as methanol To remove. This reaction product, the free-form amine of formula K-2, can be used in the coupling reaction with N-t-Boc ~ / 3-alanine / diisopropylcarbodiimide in dichloromethane. The only product under these conditions is N- (3- (cyclopropyl- (4-hydroxy-2-oxy- 5, 6,7,8,9, 10-hydro-2H-cyclooctyl [b] piperazine Uran-3-yl) -methyl) -phenyl-54-Please read the note on the back first, and then the paper size of this thread applies the Chinese National Standard (CNS) A4 (210 X 297 mm) Γ 装 83100644 Revised page of Chinese specification of patent application (August 1985) A7 _ B7 V. Description of invention (Wenduo) Employees' cooperative of Central Standards Bureau of Ministry of Economic Affairs printed diisopropylguanidine, formula κ_3, formula κ_2 and!) 1 (: Adduct of coupling agent.. L scheme consists of 3- (cyclopropylphenylmethyl) _5,6,7,8,9,10-hexahydro-4-hydroxy-2Η-cyclo [b] piperazine The homologues made by sulfide have various substituents at the 6-ct position of piperanone. The substitution at this position can be applied to good yields from the formula 3- (cyclopropylbenzene) (Kischenyl) -5,6,7,8,9,10-hexahydro-4- mesityl-2H-cyclooctyl [b] piperan-2-one trianion, (where η is 4 and! ^ Is Cyclopropyl) (formed by M2.4 equivalent of LDA) is retained by an alkylating agent. This strategy also works for 6- and 7-membered rings li * 3-. (Ring Phenylphenylmethyl) -6,7, δ, 9-tetrahydro-4-hydroxycycloheptan [b] piperan-2 (5H) -one (Formula L-1 »where η is 3 and {^ is a ring Propyl), and 5,6,7,8-tetrahydro-4-hydroxy-3- (1-phenylpropyl) -2fluorene-1-benzonan-2-one (formula L-1, wherein η. It is 2 and Rx is ethyl.) Aldehyde can also be used as the anion intermediate of the compound of L-1 (where Ri is cyclopropyl and η is 4), and it is homologous with the meridian at the α position of cyclooctyl ring. 3- (Cyclopropyl-benzyl) -4-hydroxy-10- (1-Cyclopropylpropyl Bud 5,6,7,8,9,10-Hexahydro-cyclooctyl [b] Nan-2-one (where 1-1 is cyclopropyl, 1 {2 is -0: 11 (〇} 〇 [;} 12〇113, 11 is 4). When using 1,4-diiodo When butane is an alkylating agent of a compound of formula L-1 (where (^ is cyclopropyl, ^ is 3), 9-but-3 of formula L-2 is 3-butene at the 6-ct- position -Alkenyl-3- (cyclopropyl-benzylmethyl) -4-via r ^ 6,7,8,9-tetrahydro-5H -cyclohepta [b] piperan-2-one (where R1 Is cyclopropyl, R 2 is-(CH a) 2-CH = C Η 2, and η is 3 >, which can be separated. In this example, 3 equivalents of LDA are used, I ------}; -装-/ '. ·: (Please read the note on the back first (fr page)-order-line. The paper size is applicable to the Chinese National Standard (CNS) A4 specification (2 〖〇297297mm） No. 83100644 patent application Chinese correction manual (August 1985) A7 _ B7 V. DESCRIPTION OF THE INVENTION (#) It seems that the monoalkylation is followed by the K elimination. Following a similar procedure, 8-cyclopropylmethyl-4-hydroxy-3- (1-phenylpropyl) -5,6,7,8-tetrahydro-chromen-2-one of formula L-2 (where "Is ethyl, R2 is -CH2-cyclopropyl, and η is 2) can be obtained from a compound of formula L-1 (wherein is ethyl and η is 2); and 10-cyclopropylmethyl of formula L-2 -3- (cyclopropyl-benzyl) -4-hydroxy-5,6,7,8,9,10-hexahydro-cyclooctyl [b] nanan-2-one (where 1U is cyclopropyl, 1 {2 is-(^ 2-cyclopropyl, η is 4) can be obtained from a compound of formula L-1 (wherein cyclopropyl, η is 4). The best procedure for preparing a compound of formula M-7 by Scheme M ^ (It is also a compound of formula K-2 in the K scheme) In the M scheme. The Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed under -401, K fuming nitric acid nitrates the cyclopropylphenyl ketone of the formula Η-1 A mixture of isomers of about 2: 1 can be produced. Formula M-2 desires a meta-nitro compound that can be easily fractionated from the crude mixture by recrystallization from methanol. Formula M-2 3-nitrate Catalytic hydrogenation of methylpropyl-benzone M10% Pd / C in 0¾ methanol * can produce aniline of formula M-3. The product M is separated and condensed. The amine group is then benzyl chloroformate and diisopropyl B / Dichloromethane can be protected to produce _ of formula M-4. Ketone can then be used in 5: 1 THF and ethanol to boronate kankanogen to generate the enzyme of formula M-5. Reuse formula M-5 Compound alkylation is known by the formula J-1 cyclooctylpiperone 'where η is 4, which was prepared in the J scheme-, R. Effenberger, T.

Ziegler, K.-H. Schonzoalder. ^-T. Kesmarsky, B. Bauer, Chem. Ber. 119: 3394-3404 (1986) yields compounds of formula H-6, which is also a compound of formula K1 in the scheme 。Because of this alkylation --- = ~~ — This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83100644 Patent Application Chinese Specification Correction Page (August 85) A7 ______B7 V. Invention Explanation The best condition for the (rc) reaction is para-methylbenzyl-sulfonic acid, in a refluxing diazepam, using a Soxhlet extractor containing molecular sieves. Finally, the base protecting group is dissociated in the transfer hydrogenation. -7 compounds can be obtained, which is also the compound of the formula κ-2 in the 1C scheme. The best result of this reaction can be achieved in 10% Pd / C in pure cyclohexene. 起始 The starting compound of the formula N-1, It is also a compound of formula M-7 in the μ scheme, which can be converted to a final compound of formula M-2 by coupling with -alanine, wherein the compound is 2-Ht-Boc-ethylamine. Using bis (2-oxo Methyl-3-morphidinyl) phosphine phosphonium chloride as a coupling reagent, in triethylamine / dichloromethane, 'good yield in room sowing' Into compounds of formula N-2. Using other commercially available fluorene-t-Boc amino acids, many homologs of formula H-2 can be made * and compounds of formula N-2 where h is an aryl group Carboxylic acid is completed. At the same time, the compound of formula H-2, in which 1U is naphthalene, can be prepared from the amine of formula M-1 and 1 ·· naphthoic acid, using bis (2-oxy-3-benzozine) phosphine醯 Chlorine is a coupling reagent. 0Toluenesulfonyl protective group of compound 0-1 printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Process Economics is prepared in the above procedure. N ^ Hydroxypyretriazole / THF is removed to obtain Compounds of formula 0-2. P scheme p-meta-amidamine compound pair-, wherein JU.ZNt-Boc-ethylamine or 2-ethylindole, is prepared from the 7-membered ring of formula P-1 Alkyl piperanone, made to a compound of the formula CC-4 in the CC diagram, and an appropriate carboxylic acid * using bis (2-oxy-3-oxazolidinyl) phosphine phosphonium chloride, and triethylamine / Dichloromethane. Formula __________- 57 -__ This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm> A6 __B6 V. Description of the invention (56) P-2 compound is formed in good yield under room temperature K Compounds of formula Q-2 -Diamine has divalent substituents. • Prepared from the compound of formula Q-1 * made into a compound of formula BB-2! Among them, Re2 is a benzyl group in BBK. In the progress of the reaction, you will benzyl of formula Q-2 Ammonium Mt-Boc-glycine is formed by combining bis (2-oxy-3-Dfazolidinyl) secondary gas and triethyl ether / dichloromethane * in the room. The compound of formula R-1 for the preparation of the compound of formula R-3 by R scheme is a known cyclooctylpyranone (as shown in Figure J, see formula J-1 * where η is 4 > and compound of formula R-2, It is prepared from ethylphenyl hydrazone in the following Preparation 53 in the same manner as the compound of formula Η-5 (see circle M). This alkylation reaction is performed in toluene with toluene at para-toluenesulfonic acid, and M Moderate yield yields the compound of formula R-3. The benzyloxy protecting group K10ePd / C is reached in 1: 1 cyclohexene-acetic acid to produce the compound of formula R-4. -7 is a homologue of the compound. The amine compound is then reacted with the aryl sulfonic acid to obtain a compound of the formula R-5, where 1 ^ is cyano or chlorine. At the same time, the compound of the formula R-4 is Ht-Boc-yS-alanine, The use of bis (2-oxy-3-pyridinyl) phosphanocyanine and triethylamine in ... '·. · Dichloromethane can be combined to form a compound of formula R-6. Finally, this acid amine The compound is converted to the hydrochloride salt of formula R-7 with phenol hydrochloride. ”S Printed by Shelley Consumer Cooperative, China Standards Bureau, Ministry of Process Economy (Please read the precautions on the back before filling this page). , Also M_ 中 之 M-7 Compound with phenylisocyanate ester or ethyl acetate in the reaction pickled * Μ compound of formula S-2 "is phenyl or ethyl wherein lie. -5 8 ** This paper size is applicable to the national standard i (CNS) A4 specification (210X297 mm) Printed by A6 __B6_ of the Consumer Cooperatives of the Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (57) T process type T- 2 meta-aminoformic acid compounds, where 1U is phenyl or ethyl, prepared from a compound of formula T-1 * which is also a compound of formula M-7 in M 覼 • using phenyl chloroformate or ethyl ester / Pyridine. U 潦 Formula U-1 compound, a known octylpyranone (see formula ji where η is 4) is alkylated with a compound of formula (1-2, where alkyl groups such as propyl, propyl, isobutyl Base or butyl · Made from the equivalent commercialized argon surface burying process · as described in Preparation 54. Alkylation can be generated in para-toluenesulfonic acid in the stream of methylbenzene. Compounds of formula U-3 • Among them, if they are isopropyl or propyl. V liquid formula V-1 compounds are also compounds of formula M-7 in the M plaque. A compound of formula V-2 is obtained, where IU is such as phenyl or ethyl. V is a compound of formula W-1, which is also a compound of formula Η-2 where 1U is benzyl (in Η). _In toluene • Can be converted into a sulfur homologue of formula W-2. Compounds of formula X-3 are prepared from compounds of formula X-1, known as cyclooctylpyrimidone (see formula J-1. Where η is 4 > and formula X-2 * It is prepared from isobutyrone in the same manner as in the preparation of 62K, such as M-5 compound (see M side). Alkylation reaction -Toluenesulfonic acid Benzyl oxide {谙 Please read the precautions on the back before filling in this page} -Packing L · -59- This paper size adopts China National Standard (CNS) A4 Specification (210X297) "Patent Application No. 83 100644 Chinese Revised pages of the manual (August 1985) V. Description of the invention (Resolved the problem of the printed base protection group of the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, and generated the amine of type X-4 using 10% Pd / C in a 1: 1 loop. In hexene-ethanol, this amine compound is then reacted with arylsulfonyl chloride to obtain a compound of formula X-5, where h is 4-chlorobenzene, 4-cyanobenzene, or N-methyl-imidazole. The commercial amine of Y-1 is protected by benzyl chloroformate and sodium bicarbonate in THP / aqueous solution to form a compound of formula Y-2. The aldehyde of formula Y-2 is then reacted with a Grignard reagent to produce formula Y -3 "secondary alcohol, where h can be many alkyl groups, including propyl, cyclopropyl, isopropyl, butyl, isobutyl, and allyl. The alcohol of formula Y-3 is reused for alkylation It is known that the formula Y-4 cyclooctylpiperanone is the same as the formula J-1, wherein η is 4 * in refluxing toluene and para-toluenesulfonic acid to obtain the compound of formula Υ-5. Benzyloxy The protecting group uses 10% Pd / C to dissociate in cyclohexene * to form an amine of the formula Υ-6, which reacts with an arylsulfonyl chloride to form a compound of the formula Y-7, in which the fluorenyl group and R2 is Such as 4-chlorobenzyl or 4-cyanobenzyl. Process Z Sulphonium and base, such as pyridine / dichloromethane treatment of the amine of formula Z-1 can produce sulfonamide of formula Z-2, Where Re. Is 4-nitrophenyl. These sulfonamides K are further modified by standard literature methods obvious to those skilled in the art to form sulfonamides of formula Z-3. Where Rei is such as 4-aminophenyl, and others Easy to get from the functional group of sulfonyl chloride. Such as H- [3- [cyclo-propyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperidin-3-yl ) Methyl] benzyl] -4-nitro-benzenesulfonamide nitro • K Pd / C in ethyl acetate for catalytic hydrogenation and the original * RJ generated from 4-amino-N- [3 -[Cyclopropyl (5,6,7,8,9, (Please read the notes on the back before filling out this page). Packing., Ιτ The size of the paper is applicable to the Chinese National Standard (CNS) A4 specifications ( 210X297 mm) No. 83100644 Patent Application Chinese Specification Revision Sheet (August 5 years) 5. Description of the invention (tf) 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctane [b] _pipe Alan-3-yl) methyl] phenyl] -benzenesulfonamide is an amine. Meanwhile, 3-[[[3_ [cyclopropyl (5,6,7,8, 9.10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] -piperan-3-yl) Methyl] phenyl] amino] sulfobibenzylcarboxylic acid, carboxylic acid M, methanol, and disseminateable sulfate, can be generated in 3-[[[3- [cyclopropyl (5,6,7,8 Of 1,9,10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] manan-3-yl) methyl] phenyl] limyl] sulfonyl] -benzoate Methyl ester. Sulfonamide of formula Z-3 is also obtained from the compound of formula Z-2, which further completes the reactive functional group. For example, 3-limyl-H- [3- [cyclopropyl (5,6,7,8,9,10-hexafi-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan -3-yl) methyl] phenyl] -¼sulfaminamide amines · React with benzyl chloride and bases, such as pyridine, to form H- [3-[[[3-cyclopropyl (5,6 , 7,8.9.10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfonyl] hexyl] -benzyl Benzamidine in amidine. Using commercially available sulfonium chloride, additional compounds of formula I of the present invention can be prepared, in which R20 is part of formula III, and R5 is a substituent from i) to gl), and 5U is -ΗΗΛΟζ-ο ΑΑ scheme The enantiomer of the compound of the formula AAA-1 was printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs to illustrate the enantiomers of the compound of the formula AAA-1, and was separated by chromatography using a pair of palm HPLC. The separated enantiomers (formulas Α-2 and Α-5), whose protective group K catalyzes the removal of hydrogenation, can produce pure amines on the enantiomers of formula A Α-3 and A Α-6. AA-3 and AA-6 respectively react with sulfonium and base- (such as pyridine) to form sulfonamides A A-4 and A A-7, of which Re. Is such as 4-Guphenyl. Using commercially available sulfonium chloride, additional compounds of formula I of the present invention can be prepared, where R10 and R20 are part of formula III, and where Rs is a substituent from i) to gl), and χ; _ _ _- 61 -This paper size applies Chinese National Standard (CNS) A4 specification (210 × 297 mm) ^ A6 __B6_ V. Description of the invention (60) -N -SOz- ° BB process BB-2 amine is shown in 8B plaque. The amine BB-1 is condensed with an aldehyde, and an aldehyde such as benzaldehyde or phenethylaldehyde, and the imine formed by the amine reacts with sodium argon to form an alkylamine of formula BB-2, where Re2 is a benzyl group. The BB plaque also describes the sulfonation of BB-2 N-alkylamines. • It reacts with commercially available sulfonium chloride and is catalyzed by K sugars (such as pyridine) to form sulfonamides of formula BB-3. Among them Rei Is, for example, aryl, aryl, or substituted aryl * and Re: / is benzyl or alkyl. CC Scheme Amine of CC-5 was prepared as described in the CC circle. Compounds of formula CC-2 K Compounds of formula CC-1 / methylbenzine • Treatment under room rent and addition of para-toluene sulfuric acid can produce cycloheptylpyrans protected by formula CC-3 Cbz. After protection, an amine of formula CC-4 can be formed. The amine is treated with sulfonium and sickle (such as pyridinium methane). • Sulfaline of the formula CC-5 * can be formed, where Re0 is such as 4-cyanophenyl. DD Scheme DD illustrates the oxidation of the jR group in a compound of formula DD-1. This compound is oxidized in DMS0 · M potassium carbonate and hydrogen peroxide solution to form amidine of formula DD-2. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Process Economy {Please read the precautions on the back before filling in the pages) • Install-^-type ΕΕ-1Μ amine (such as morpholine) in the submerged ethyl acetate and add Treatment with sodium iodide yields a cyclized product of formula Ε-2 and a coded formamidine sulfonamide * of formula Ε-3 and a hydrogen iodide salt of formula Ε-4. _6 2 _ This & scale is applicable to the National Standard for Chlamydia (CNS) A4 (210X297 mm) No. 83100644 Patent Application Chinese Specification Correction Page (August 85) A7 _____ B7 V. Description of the Invention (^) Commercial formula Cyclopropylthiophene-2-ylmethanol of formula FF-1, reacted with piperanone of formula FF-2 in dichloromethane and catalytic fluoroacetic acid (TFA) * to produce compound of formula FF 3- (α-cyclopropylthiophen-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperanone. GG Scheme Commercial thiophene 2-carboxaldehyde of formula GG-1, treated with M ethylmagnesium bromide / ether at room temperature, can produce methanol of formula GG-2. " -Mixture of formula GG-2 and formula GG-3 / dichloromethane, M-catalyzed TFA treatment can produce 3- (ot-ethylthiophen-2-ylmethyl) -4-hydroxy-5, of formula GG-4, 6, _7] 8, 9, 10-hexahydrocyclooctane [b] sulfan-2-fluorene. HH process Commercially available 5-methyl-2-carboxaldehyde thiophene of formula HH-1, K ethylmagnesium bromide / ethyl treatment at room temperature can produce methanol of formula HH-2. HH-2 methanol of formula HH-3 / dichloromethane mixture, treated with catalytic TFA can produce 3-U-ethyl- (5-methylthien-2-ylmethyl) -4 of formula HH-4 -Hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one. Scheme II Commercialized benzothiophene M n-butyllithium / THF of formula II-1, processed at room temperature. Adding cyclopropanecarboxaldehyde to the previous solution can produce a formase of formula II-2. Mixture of formula III-2 and formula 11-3 piperanone in dichloro # alkane, TFA treatment with K catalyst amount "can generate 3- (α-ethylbenzythiophene-2-ylmethyl) of formula II-4 Group) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-copper. JJ process ---______- 63- This paper size is applicable to the Chinese National Standard (CMS) M specifications (210 乂 297mm No. 83100644 patent application Chinese manual amendment page (August 85) A7 ______ B7__ V. Invention Explanation (Commercial formula of JJ-1 furanmethyl-2-yl alcohol, M2 equivalent of n-butyllithium / THF is treated at room temperature. Cyclopropanecarboxaldehyde is added, and the reaction is stopped with dilute acid. This formula JJ- Diol of 2. Glycol of formula JJ-2 and piperanone of formula JJ-3 • M-catalyzed TFA / dichloromethane treatment at room temperature * can produce compound of formula JJ-4, 3- (cx-cyclopropane (5-hydroxymethylfuranmethyl-2-yl) -4-meryl-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2- 嗣. Commercialization of KK process Formula KK-1 2-Thienylmethanol, M 2 equivalents of n-butyllithium are treated in THF * at room temperature. Cyclopropanecarboxylic acid * is added and the reaction M dilute acid is stopped. This produces the second enzyme of formula KK-2. Formula A diol of KK-2 and a mixture of formula KK-3 piperanone, PK-catalyzed TFA / dichloromethane, and treatment at room temperature * can produce a compound of formula KK-4, 3-U-cyclopropyl ( 5-hydroxymethylthien-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] Uran-2-one 0 LL Printed a commercial formula of LL-1 2-thiophene ethanol by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Process Economy, K 2 equivalents of n-butyllithium were processed in THF 'at room temperature. Cyclopropane carboxyl Aldehyde and K dilute acid to stop it. This produces a diol of formula LL-2. A mixture of LL-2 diol and LL-3 copper piperane is treated with catalytic TFA / dichloromethane at room temperature, It can form compound 3- (α-cyclopropyl (5- (2-hydroxyethyl) thiophen-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10- Hexahydrocyclooctane [b] piperan-2-one. MM scheme "M-2 compounds can be prepared from the commercial formula MM-1, furan methyl fermentation, such as Bull. Cheat. Soc. Jpn., 65U) , 1992 and Zh. 〇rg.

Khim, 25 (4), 843-6 (Russ), 1989. The compound of formula MM-2 is treated with n-butyl lithium and then added with cyclopropanecarboxaldehyde to form a compound of formula MM-3 ____- 64 -_____ This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm), Revised page of Chinese Specification for Patent Application No. 83100644 (August 85) A7 B7 V. Description of the invention (ο) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 0-form MM-3 compound and MM-4 piperan Mixture, treated with M-catalyzed TFA / dichloromethane to yield a compound of the formula MM-5, 3- (α-cyclopropyl- (5- (2-hydroxymethyl (methoxymethyl ether)) furanmethyl-2 -Yl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one. NN scheme HH-2 compound prepared from the commercially available xanthen-2 -Alcohol, NH-1, such as Bull. Chem. Soc. Jpn., 65 (9), 1992 and Zh. Org. Khim, 25 (4), 843-6 (Russ), 1-9 89. Compounds of formula HH-2 K n-butyl lithium treatment, and then add cyclopropylcarboxaldehyde M to form a compound of formula-3. Compound of formula NN-3 and piperane K of HH-4 K catalytic TFA / dichloromethane treatment to generate compound of formula NN-5 , Which is 3-(α-cyclopropyl (5- (2-hydroxymethyl (methoxymethyl ether) thiophene-2- (Methyl) -4-hydroxy-5,6,7,8,10-hexahydrocyclooctyl [b] manan-2-moe. 00 Scheme benzyl ester chloride is added to NaHC containing furanamine of the formula 00-1. 3 Saturated solution was added with stirring and stirring. After extraction with ether, the solvent was removed under vacuum to isolate the product of formula 00-2. The compound of formula 00-2 and the cyclopropylcarbonyl atmosphere / methylene chloride complex , K excess aluminum chloride treatment. This produces a compound of formula 00-3, compound of formula 00-3 MHaBH4 is treated in an ethanol / THF mixture, followed by M acid operation to generate a compound of formula 00-4. Compound of formula 00-4 and Treatment with piperanone * KTHF / dichloromethane of formula 00-5 yields the title compound of formula 00-6, 3-(α -cyclopropyl (5-(fluorenyl-phenyl ester phenyl) methyl) ) Furanmethyl-2-yl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctane [b] piperan-2-copper. ____- fi R-This paper is for China National Standard (CNS) A4 Specification (2 丨 OX2? 7mm) (Please read the cautions on the back before filling in this page) Binding · Bookmarking No. 83100644 Patent Application Chinese Manual Correction Page (August 85) A7 ____ B7 V. Description of the invention (PP process benzyl ester chloride in It was added to a vigorous stirring of formula PP-1 2- thienyl Ha HC03 amine of the saturated solution. After extraction with K ether, the solvent was removed under K to separate the product of formula PP-2. A mixture of a compound of formula PP-2 and cyclopropylcarbonyl chloride / dichloromethane is treated with K excess lithium chloride. This produces a compound of formula PP-3. Compound KHaBH4 of formula PP-3 is treated in an ethanol / THF mixture, followed by acid treatment to form an ether of formula PP-4. Mixtures of compounds of formula PP-4 and piperane of formula pp-5. M TPA / dichloromethane treatment yields compounds of formula PP-6, 3-U-cyclopropyl (5- (N-benzyl ester benzyl) amine (Methyl) thien-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrooctyl [b] piperan-2-copper. QQ process The commercialized formula of furanylamine QQ-1, M2 equivalent of n-butyllithium / THF is processed under room temperature. To this solution is added cyclopropanecarboxaldehyde, which forms an amino alcohol of the formula PP-2. An alcohol of formula QQ-2 and a mixture of 4-fluorobenzenesulfonyl chloride / dichloromethane and K triethylamine treatment can produce sulfonamide of formula QQ-3. Mixture of a compound of formula QQ-3 and piperanone of formula XX-4, treated with M-catalyzed TF A / dichloromethane to produce a compound of formula QQ-5, 4-fluoro-N- [5- [cyclopropyl (5 , 6,7 ,. Printed by 8,9,10-hexahydro-4-hydroxy-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] Furan-2-yl] benzenesulfonamide. RR scheme A compound of formula RR-1 and a mixture of 4-cyanobenzenesulfonyl chloride / dichloromethane are treated with triethylamine to form amidamine of formula RR-2. A mixture of a compound of the formula RR-2 and a piperanone of the formula RR-3, treated with M-catalyzed TFA / dichloromethane to produce a compound of the formula RR-4, 4-cyano-N- [5- [cyclopropyl (5 , 6,7,8,9, __-66 -_ This paper size is applicable to the Chinese National Standard (CNS) A4 size (210x297 mm) No. 83100644 patent application tired Chinese manual amendment page (August 85) A7 _ Β7 5. Description of the invention u 乂) 10-hexahydro-4-hydroxy-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] furan-2 printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs -Yl] benzylamine. SS process Commercialized 2-thiophene limb of formula SS-1, treated with 2 equivalents of n-butyllithium / THF at room temperature. To this solution was added cyclopropanecarboxaldehyde, which produced an amino alcohol of formula SS-2. A compound of formula SS-2 and a mixture of 4-fluorobenzenesulfonyl chloride / dichloromethane are treated with triethylamine to form sulfonamide of formula SS-3. Compounds of formula SS-3 and piperane-stick compounds of formula SS-4, treated with catalyzed TFA / digas methane * to produce compounds of formula SS-5, 4-fluoro-N- [5- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-oxy '-2-2H-cyclooctyl [b] piperan-3-yl) methyl] thiophen-2-yl] benzenesulfonate Lamine. TT scheme A compound of formula TT-1 and a mixture of 4-cyanobenzenesulfonyl chloride / dichloromethane and M triethylamine can produce sulfonamide of formula TT-2. Mixture of compound of formula TT-2 and formula TT-3 piperanone K Catalytic TFA / dichloromethane treatment yields compound of formula 1'-4, 1 <-[3- [cyclopropyl (5,6,7 , 8,9,10-hexahydro-4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3-yl) methyl] thiophen-2-ylmethyl] 4-cyanobenzenesulfonate Lamine. The UU process is commercialized with the formula UU-1 2-phenanylmethanol M2 equivalent of n-butyl lithium, and then methyl iodide is added, and then another equivalent of n-butyl lithium and cyclopropanecarboxaldehyde are added to form the formula UU. -2 glycol. The compound of formula X-2 and the piperinone formula UU-3, treated with TFA / dichloromethane in the amount of M catalyst, can generate the compound of formula ϋϋ-4, 3- (ct-cyclopropyl (5-methyl -4 -Hydroxymethylthiophene-2 -—_: _- 67 -_ This paper size is applicable to the Chinese National Standard (CNS) M specification (210 > < 297mm) (Please read the precautions on the back%) (Fill this page)-Binding. Binding No. 83100644 Patent Application Chinese Specification Revised Page (August 85) V. Description of the Invention (Methylmethyl) -4-hydroxy-5,6,7,8,9, 10-hexahydrocyclooctyl [b] piperan-2- 喃. VV Scheme 2-Ethylcyclooctanone, prepared as described in Organic Synthesis, Vol. 47, p 20. 2-Ethylcyclooctyl嗣 K sodium hydroxide treatment can generate lu-keto acids of formula VV-1. Compounds of formula VV-1 can be treated with a catalyst amount of osmic acid / acetic acid and acetone to produce intermediates of formula VV-2. Formula VV-3 The treatment with 3 [R] -phenylpentyl oxalochloride / dichloromethane can generate a hydrazone atmosphere of formula VV-4. A mixture of a compound of formula VV-2 and triethylamine is added to a reflux solution of formula VV-4 (1,3,5-trimethylbenzene), which can generate compounds of formula 7 \ [-5, [$]-3- (ethylbenzyl) -5, 6,7,8,9,10-hexahydro-4-¾yl-2H-cyclooctyl [b] piperan-2-one. WW process formula WW-3-3 [S] -benzyvaleric acid K mono Treated with ammonium chloride / dichloromethane, a fluorenyl chloride of the formula WW-4. A mixture of K triethylamine and a compound of the formula M-2 can be added to a reflux solution of the compound of the formula WW-3 (1,3,5- Trimethylbenzene) to form compounds of the formula WW-5 "[R] 3- (ethylbenzyl> -5,6,7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctyl [b] Piran-2-one. XX Unsaturated ammonium amines (Chemistry Letters (1981, 913-16) K-dimethylmagnesium bromide / diethyl ether) printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Process Economy At -40 t: the compound of formula 父 -2 can be formed. The acid hydrolysis of the compound of formula 乂 ¥ -2 can generate the intermediate of formula 义 -3. M is similar to the above method. Phenylmagnesium bromide / diethyl ether treatment can produce compounds of formula XX-5, which once treated with an ester can form intermediates of formula XX-6. Compounds of formula XX-3 and formula XX-6, wherein the phenyl group is as _.__. _- 6 8 ~ __ This paper size is applicable to Chinese National Standard (CNS) Α4 size (210x297 mm) Central Standards Bureau of the Ministry of Economic Affairs®: Industrial-consumer cooperation Printed A6 B6 V. Description of the invention (6?): Halogen, bluefluoromethyl, -HHBOC, -HHCOBz, -HHS02Ph or (1,1,4,4-tetramethyl-1,4-bisdisiloxane) Ethyl) substitution (for example, see compound 22-5 in 22) or phenyl M depending on the substituted heterocyclic ring, such as furan and sialphine, can be prepared after the above steps. Unsaturated fermented amines of the formula U-1 (Hurby, et. Al., J. Org. Chea. (1993) 58, 766) W Phenylmagnesium bromide in the presence of ketone-catalyzed two / tetrahydrofuran. To produce compounds of formula YY-2. Hydrolysis of a compound of the formula YY-2 produces a compound of the formula YY-3 (same as the compound of the formula XX-6 in the XX plane). In a similar manner, compounds of formula YY-4 are converted into compounds of formula YY-5 * and finally converted to compounds of formula （-6 (same as formula XX-3 in XX). Compounds of formula ΥΥ-3 and ΥΥ-6, in which benzene The group is substituted by halogen, trifluoromethyl, -HHB0C, or -NHCBz, or the phenyl group is substituted by a heterocyclic ring such as furan and thiophene depending on the box, and can be prepared according to the above method. At the same time, * compounds starting from formulas ΥΥ-7 and ΥΥ-8 * can be used to prepare compounds of formula ΥΥ-3 and ΥΥ-6 in this way. The ethyl group is replaced by cyclopropyl. ZZZ process The fermenting acid of formula ZOZ-1 is treated with 2 equivalents of lithium hydrazone diisopropyl-amine / tetrahydrofuran. To this solution is added cyclopropanecarboxaldehyde (available from G &T;. After the aqueous hydrocarbon treatment, racemic compounds of the formula ZZ-2 can be separated. Kot-methylbenzylamine, ephemic acid, ephedra "I, The RjgS isomer of Jinzixian, Panmuyan_, Jinning, Jinjitin, Quannidine, or Jinjining crystallized in Mitufen, and the [R] isomer of formula ZZ-2b and formula [S] isomers of ZZ-2a. In addition, * Ivantian Dilue (J. Ab. Che ·. Soc. (198U 103, 2127)) {Please read the precautions on the back before filling in this page}. • ΤΓ _69_ This applies to China National Standard ^ (CNS) A4 specification (21〇χ? 97ϋ) A6 B6 V. Description of the invention (68) Fermentation synergy can also generate the pair of formula ZZ-2a and formula ZZ-2b Enantiomer. Treatment of formula ZZ-2a with triethyl ortho-acid, can produce ZZ-3 (Helv.

Chi ·. Acta. (1987) 70, 1320). Once the compound of the formula ZZ-3 is pyrolyzed, the compound of the formula ZZ-4 can be formed (Helv. Chi ·. Acta. (1987) 70, 1320). Compounds of formula ZZ-4 and compounds of formula ZZ-5 are treated in the presence of sulfonated ketene (Tetrahedron Letters 1.253 (1984)) to produce formula ZZ-6. Compounds of formula ZZ-6 are made of chlorine / diamine [[methane treatment number Hours • Compounds of formula g-7 are produced. Compounds of formula 22-7 are heated in a hot 1,3,5-trimethylbenzyl solution. • Triethylamine / toluene and a solution of formula ZZ-8 are added. The reaction is heated for several hours. " The surface is dissolved in a thin layer (silicon, ethyl acetate). The compound of formula ZZ-8 is removed by evaporation when it is completely consumed. In this way, a compound of the formula ZZ-9 is formed. Para-methylbenzyl sulfonic acid and daumannmann's formic acid treatment can produce compounds of formula ZZ-10. The methane solution of formula ZZ-10 is confirmed by the presence of triethylamine and M-para-cyanobenzene. Gas treatment * can generate compounds of the formula ZZ-11. Male compounds, compounds of the formula ZZ-3 and compounds of the formula ZZ-5, in the presence of gullized subarsenic δ (Tetrahedron Letters 12 · 5 3 (1984)) can generate the formula ZZ -12 compounds, the enantiomeric formula of the formula ZZ-έ 彳 b, and when carried out in a similar manner to ZZ-6 can generate compounds of formula ZZ-13. Furthermore, compounds of formula ZZ-14 and Compounds of formula ZZ-15 • Substitute formulas ZZ-4 and ZZ-3 compounds M to make equivalent ethyl rya isomers. Printed by the Central Consumers' Bureau of Ministry of Economic Affairs, Consumer Work Cooperatives {Please read the precautions on the back before Fill in this page)%. Treatment of ketone M (ethyl methylene) triphenylphosphine of formula ΑΑΑ-1 can generate unsaturated ester of formula ΑΑΑ-2. The original effect of the compound of the formula ΑΑΑ-2 (Red-Al -70- This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) A6 B6 Printed by the Ministry of Economic Affairs t Central Sample Standard Bureau Shellfish Consumer Cooperative Description of the invention (69) / Cubr, DIBAH / MeCu; HaBH4 / resin; NaBH4 / CuC12; see Reduction by the A1u · i no and Borohydr ides in Organic Synthesis, J. Seyden-Penne, VCH Publishers, Inc. Lavoisier-Tec & Doc, 1991, p 156) · Revisiting_ Hydrolysis can produce compounds of formula AAA-3. Racemic acid methyl benzylamine-ephedrine, ephedra, cypress, Ml, quinine, jiasonidine, quinidine, or tamagine [R] or [S] The structure is crystallized in stages to obtain [R] isomers of formula AAA-4a and [S] isomers of formula AAA-4b. In addition, the compound of formula AAA-4a and the compound of formula AAA-4b * can be obtained by 不 hydrogenation (Angev. Che ,. Int, Ed. Eng.l. (1989) 28, 60) and Λ hydrolysis . A compound of formula AAA-6, which is also a ZZ-10 compound in a ZZ garden, can be prepared in the manner described in ZZ 豳. BBB process Conversion of commercial sucrose scent BBB-1 to sulcosamine BBB-2 * It can be processed by using a suitable aromatic amine ArHH2 (commercially available or easily prepared by known methods). M-butyllithium is halogenated to gold and exchanged with the commercial cyclopropanecarboxylate to form a condensed β * intermediate. The alkylation of the prionite intermediate BB-4 with benzyl ether BB-3 can be accomplished using a variety of acidic conditions, several of which have been described in previous schemes. This produces the final product, BBB-5 ° CCC, Phosphonamide CCC-4 is synthesized from the aromatic intermediate CCC-1, which is a typical phosphine atmosphere CCC-2. The latter can be easily prepared using procedures such as those described in Tetrahedron 49: 11055 (1993). Aminophosphine _ _ {Please read the precautions on the back before filling in this page}. Packing -71- This paper size adopts China National Standard (CNS) A4 specification (210 X 297 mm) A6 B6 Ministry of Economic Affairs The Central Bureau of Standards, X. Consumer Cooperatives, India, V. Invention Description (70) CCC-6, which is made by the treatment of an excessive amount of aromatic amine intermediate CCC-1M and sickle phosphine dichloride. (Dichloride can be synthesized by the method of Buying 1 or using Organic Phosphorous Compounds, G.M. Kosolapoff and L. Maier, eds., Vol. 4, p. 155-253 (1972 >). The resulting intermediate CCC-5M «When the enzyme R 'OB can be converted into amino amine acid _ CCC-6. In addition, the general route of the amino phosphonate of formula CCC-6 is reported in Bi ganganic and medicina IC heistry, V ο 1.2 »1047 (1992) 〇 DDD process Aromatic amines (DDD-1) in the aromatic amines can be derived from the sulfonium gas DDD-2 (available commercially or according to J. Org. Chen. 41: 4028 (1926) or J. Med. Chen. 1 5: 538 (1972), and easily converted to sulfosaccharid gland DDD-3 ° It can be clearly understood by ordinary artisans that the compounds of the present invention can It exists in several diastereoisomeric forms • It depends on the configuration of the asymmetric carbon tetrazen. All the diastereoisomeric forms are included in the garden of the present invention. At the same time, the compounds of the present invention There are several types of 4-hydroxy-pyridine ring tautomers in Koli. These include the special fermented form of M form I and the special form shown in formula VI. And its conjugates. All such tautomeric forms are included in the scope of the present invention. The compounds of the present invention may be in the free form, or the remaining (non-previously protected) carboxyl, amine, monovalent M Types of protection / protection on radicals, hydroxyl groups, or other reactive groups. The protecting group can be any one known in the art. Examples of nitrogen and oxygen protecting groups are in TW, Greene, Prote ting Groups in -72, this paper standard逋 Using China National Standard (CNS) A4 specification (210X297 public love ·) < Please read the precautions on the back before filling in this page}. Installed by the Central Bureau of Standards, Ministry of Economic Affairs, Paiton Consumer Cooperatives, A6 B6 V. Description of the invention (π)

Organic Synthesis, Viley. Hew York, (1981)? J.F.W. HcOnie, ed. Protective Groups in Organic Chenistry, Plenu 臞 Press (1973) and J. Fuhrhop and G. Benzlin, Organic Synthesis, Verlag Cheaie (1983). Included among them are 5-butanilino (B0C >, benzyloxy, ethyl ethyl, allyl, phthalofluorenyl, benzyl, benzamidine, tritylmethyl and others. The present invention provides Compound I or its pharmaceutically acceptable hydrazone and / or hydrate. The pharmaceutically acceptable salt will hold it to the chemical manufacturing chemist and the parent compound is equivalent in nature under K. , Stability, patient acceptability, and bioavailability. Examples of such K include argon tfi acid, such as gadolinium and hydrogen moth salts, sodium and potassium salts. The compounds of the present invention can be used to treat human immunodeficiency virus (HIV) infected patients, which cause AIDS and related diseases. In this case, these compounds can be administered through the mouth, eye, nose, percutaneous, subcutaneous and parenteral (including intramuscular and intravenous) routes.剂量 The dosage is from 0.1 gram to 100 milligrams per kilogram 髑 day weight. The skilled artisan should know that the chemical compound of the present invention is thus blended into a suitable scholastic cocoon form. Examples of the dosage form include oral and eye humor Such as lozenges and capsule cocoons, or exogenous blends such as sterile solution cocoons. Hours • Effective amount is from about 0.1 g to 100 mg per kilogram of weight per day. Both solid and fluid forms can be made for mouth and eyes. The solid composition is prepared by compounding the compound of the present invention with traditional forms. And other blends, such as talc, magnesium stearate, dicalcium phosphate, magnesium aluminum silicate, calcium sulfate • Yodo-73- This paper size uses Tai® Home Standard (CNS) T4 specifications (210X297 mm) ... ........................................ ... 0 ............ installed ............玎 .................. k {Please read the notes on the back before filling in this page} _ A6 __B6_ V. Description of the invention (72) Powder, lactose, gum arabic , Methyl cellulose, or a functionally equivalent medicinal diluent and carrier. Capsule noodles are prepared by mixing the compound of the present invention with eucalyptus dilute cocoons. Preparation of soft and bright sleeping lumbar sac cocoons A pseudo-packing of a compound of the present invention with an acceptable base oil * such as vegetable oil or liquid petroleum ether of tincture is performed. The preparation of cocoons is based on the invention Compounds are soluble in aqueous solvents It is made by adding sugar, aromatic fangfanlang and Baoying. Awake _ preparation of Langley _ water solvent, such as acetonitrile, painful sweetness _ such as tincture or saccharin, and aromatic fragrant cocoons. Suspension _ of The preparation is based on aqueous solvents and suspension aids, such as rapabolic, tragacanth, or methylcellulose. When the compound of the present invention is administered externally * it can be injected or injected intravenously. Effective cocoon The daily pulp weight per kilogram is from about 0.1 mg to 100 g. The preparation of Tengwai solution is prepared by dissolving the compound of the present invention in an aqueous solvent. * After aseptic filtering, it is placed in a fusion-sealable vial or ampoule. . The method for preparing parenteral suspensions is practically the same, except that a sterile floating agent vehicle * is used and the compound of the present invention is sterilized with K-oxyethane or a mixed gas before being suspended in the vehicle. The exact route, placement, and release frequency can be easily determined by the artist based on the patient's age, weight, general health conditions, or other bed symptoms. 0 Printed by the Consumer Cooperatives of the Standard Bureau Staff of the Ministry of Economic Affairs {Please first Read the notes on the reverse side and fill out this page)-The patients who are accepted for treatment are the following: 1) Those infected with a human immunodeficiency virus virus on MG * K is determined by the presence of detectable virus antibodies or antigens in the serum, And 2 > is asymptomatic HIV infection or symptomatic AIDS clear infection • such as 丨) diffuse sister plasmosis, ϋ > is a psoriasis, twist -74- This paper uses the national standard of t CNS) A4 size (210x297 mm) A6 __ B6_ V. Description of the invention (73) 1 bronchial and pulmonary candidiasis, including pneumocystic pneumonia · iv > non-Hawkinson's lymphatics, or V) card Bosi's meat scan and 60 years old M; or the absolute number of CD4 * lymphocytes in peripheral blood and less than 500 /? 3. Treatment includes maintaining the level of inhibition of the compounds of the present invention at all times * and can be continued until a second symptomatic AIDS infection is clearly manifested and a different therapy is indicated. The usability of the compounds of the present invention is demonstrated in the following biological tests: Based on the results of the HIV protein sea sieve analysis and the fluorescence test, it can be used with special beads coated with avidin. Undissolved in the dissociation product. The substrate was biotinylated on the amino acid-containing spermatozoa acid, and M-fluorescein isothiocyanate (FITC) fluorescence was recorded on the lysine acid on the carboxyl terminal. This analysis has been used to detect novel non-peptide inhibition of HIV-1 protease. The mass (0.2w Μ of 20 liters), sample (10 microliters of desired concentration), and enzymes (0.1 «M of 10 liters) were added to a 96-hole Pandex disk. Analysis was performed at 0.1 of PM5.5 In Μ sodium acetate buffer solution • Performed in the presence of 1.0 MM sodium and 0.05% HP-40 * and incubated for 1 hour at room temperature in the dark. Then add streptavidin-coated polybenzyl bead beads (0.1¾ (w / v >, 40 liters), and set the plate in a dark room for another half an hour. The hunger-causing product from the unreported Separation by quality in case of filtration • Read out in the Index screening machine. Analyze the data using a combined electrical algorithm to determine the percentage of inhibition. Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the back first) Note on re-filling this page} The determination of the value uses the same materials and equipment to study the percentage of inhibition and inhibition. For certain inhibitors from 3 or 4 initial concentrations, make 2 times serial dilutions for a total of 24, 36 or 48 Individual dilution concentrations are employed. These dilutions use -75 · Zhang scales applicable to National Standards (CNS) A4 specifications (210X297 mm) A6 B6__ V. Description of the invention (74)

BioMek splash manipulator system. The analysis included 10 µl of 40 r »M HIV-1 protease, 10 µl of various inhibitors, and 20 µl of 200 ju M substrates (40 µl total). The reaction was performed at room temperature for 90 minutes, and the suspension was stopped by adding 40 microliters of anti-biocides such as anti-biotics (see above). Performed in parallel with known IU inhibition S! Credibility. Data are modified by computer programs * Nonlinear least squares analysis of the data can be used to generate IU values.% Inhibition of representative compounds of the invention, and in some cases ICB0 or K / value * In the following Tables I and IV. The compounds of the present invention have been further evaluated in the CV-1 cell analysis below * where it has been shown that the retroviral-inhibitory effect is due to the inhibitory effect of the HI V-1 protein. Economy Printed by the Department of Consumer Standards of the Central Bureau of Standards {"Precautions for reading the back and then filling the nest page"} In vVK-1 infected CV-1 cells, there is an inhibitory effect of p55 treatment modification. CV-1 cells per The holes 2xlOsffi cells were seeded in 24 holes of Costar trays, and then 4-6 hours later vVK-1 was infected by 5th plaque forming unit (PFU) per cell. Each compound was dissolved in 2.5% embryo bovine serum Dulbecco's Modified Iller's Medium (DMEM) · 2 hours after virus addition The final concentration is added to the repeated holes. After 24 hours • Remove the culture medium and wash the army IS with K 1 ml of PBS buffered water (PBS), and add 0.1 liters of filler slow street solution (62.5 »H See hydroxymethylaminomethane (1 > 13 >, 1 «6.8, 2.3% sodium dodecyl sulfate (503 >, 5% / 3-thioglycollase, and 10% glycerol). Do not collect lysates, Place in boiling water for 3 hours, and take 0.025 liters of each sample to receive _ electrophoresis of 12% SDS-polyacrylamide gel. Peptone electrophoresis is stained to nitrification, and the protein is analyzed by immunoassay. First The antibody is a P24 goat antibody (International -76- This paper uses 1 »National Standard (CNS) A4 Specification (210X297 mm) No. 83100644 Patent Application Chinese Specification Correction Page U5 Aug. 5) A7 V. Description of the Invention (7,0 Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs

Enzyne. Inc., Fallbrook, California) and the secondary antibody was a pro-phospho-conjugated rabbit-goat-rabbit G antibody (kirkegaard & Perry Laboratories, Gaithersburg, Maryland). The densitometer (Bio-Rad, Model 26 0) was used to quantify the level of rabbit disease-reactive protein with the 1-D analysis software of the associated risk. Inhibition refers to a decrease in the average percentage of P24 levels * as determined by repeated drug-treated samples compared with untreated drug-treated controls. In general, there must be no change in the percent inhibition rate during repetition. It was also determined in each experiment that the Klw Μ peptide Hoa-His-Cha PSI [CH0HCH0H] Va and Ile- / Up-treated cultures were used for the production of p24, and this peptide is also known as H- [1- (Cyclohexylmethyl) -2,3-dihydroxy-5-methyl-4-[[[2-methyl-1-[[(2-pyridylmethyl) amino] carbonyl] butyl]- Amine] carbonyl] hexyl] -α-[[(1-naphthyloxy) ethenyl] amino-, [lS-ClR-UyjS'SS *, 45! * (11 ^, 21 ^)]]- 1 Bimizole-4-Propanamide) (which has been disclosed in the international case Ho. W0 87/05302 * published on September 11, 1987). Percent inhibition values for representative compounds of the invention are shown in Table III below. M is the preferred compound of the present invention: Ν- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b ] Piperan-3-yl) methyl] phenyl] -benzenesulfonamide only- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2- Oxy-21 ^ -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-ethylenesulfonamidocarbamic acid, [3-[[3- [cyclopropyl ( 5 ^ 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -3- Ketopropyl] -1,1-dimethylethyl ester (Please read the note on the back _ then fill in this page)-Packing. Thread ---------- 7 7 a paper Standards are applicable to Chinese National Standard (CNS) A4 specifications (210X297 metric whole) No. 83100644 patent application Chinese manual amendment page (August 85 > A7 B7 V. Description of invention () Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Ν- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2} 1-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -propanesulfonic acid N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-methyl-benzenesulfonamide N- [3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-21 {-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -1-butanesulfonamide 4-N- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-_yl-2H-cyclooctyl [ b] piperan-3-yl) methyl] benzene_; yl] -benzenesulfonamide H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxyl -2-oxy-2} 1-cyclooctyl [b] piperan-3-yl) methyl] phenyl f-2-naphthalenesulfonamide 3,4-dichloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonyl Amine N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl Yl] phenyl]-(R) -benzenesulfonamide (-)-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxo -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-[(E)]-ethylenesulfonamide (+) -N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-benzyl -[(E)]-ethylenesulfonamidoaminocarboxylic acid, [2-[[3-cyclopropyl (5, name, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy -2H-cyclooctyl [b] piperan-3-yl) group] phenyl] amino] -2 -Oxyethyl]-, 1,1-dimethylethyl ester aminocarboxylic acid * [2-[[3-cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxyl __- 78 -_ This paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) (Please read the note on the back '^ before filling this page)-Binding & Thread No. 83100644 Patent Application Revised page of Chinese manual (δ5 years in August) A7 B7 V. Description of the invention Π /) Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs, 2-oxy-2H-cyclooctyl [b] piperan-3-yl) A [Phenyl] phenyl] amino]-(1H-oxazol-4-ylmethyl) -2-oneethyl]-* 1,1-dimethylethyl ester N- [3- [cyclopropyl | : 5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-fluoro- Benzsulfonamide 4-bromo-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) methyl] phenyl] benzenesulfonamide H- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy- 2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] "-4" nitro-benzenesulfonamide N- [3- [cyclopropyl (5,6,7,8,9 , 10-hexahydro-4-hydroxy-2-oxy-2 {{-cyclooctyl [b] piperan-3-yl) methyl] benzene Γ-3-nitro-benzenesulfonamide H- [3- [cyclopropyl (5,6,7,8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-methoxy-benzenesulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexa Hydrogen-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- (trifluoromethyl) bensulfonamide K- [3- [ Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-21] -cyclooctyl [b] piperan-3-yl) methyl] phenyl]- 2,4-difluoro-benzenesulfonamide 3-n-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H -Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-propanesulfonamide 4-cyano [cyclopropyl (5,6,7,8,9,10-hexahydro- 4-Hydroxy-2- 2-yl-2cyclooctyl [b] piperan-3-yl) methyl] phenyl] benzenesulfonamide 4-cyano-N- [3- [cyclopropyl (5, 6,7, · 8,9, 10-hexahydro-4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3-yl) formamidine] phenyl] -benzenesulfonamide Salt H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2v-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -8-quinolinesulfonamide _: _- 7 Q -_; _ This paper size applies to China National Standard (CMS) A4 specifications. (210X297 mm) (please Read the back of the drive precautions # reloading the page)

I-Pack. Binding Line No. 83100S44 Patent Application Chinese Specification Revised Page (August 85) A7 B7 V. Description of Invention (Aminocarboxylic acid, [2-[[3- (R or S)-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -2 -Fluorenylethyl]-, 1, dimethyldimethylethyl ester N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2 ^ 1 -cyclooctyl [b] piperazin-3-yl) methyl] phenyl] -2, 1,3-benzothiadiazole-4-sulfonamide 3-chloro-N- [3- [ Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-keto-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -benzene Sulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] phean-3-yl ) Methyl] benzyl f-4-benzofurosulfonium 3-bromo-H- [3- [cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy- 2-keto-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide 3-[[[3- [cyclopropyl (5,6,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -benzylcarboxylic acid (+)- 4-chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piperan-3-yl) methyl] phenyl] -benzenesulfonamide (-)-4-chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexa Hydrogen-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (+) -4-cyano-N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- Benzylsulfonamide (-)-4-cyano-N- [3- [cyclopropyl (5, · 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2Η- Cyclooctyl [b] piperan-3-yl) fluorenyl] phenyl] -benzenesulfonium N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxy-2-oxy-2H -cyclooctyl-3-yl) methyl] phenyl] -1-methyl- (S) -1H-imidazole-4-sulfonamide_-80 -__ Applicable to this paper size Chinese National Standard (CNS) A4 Specification (210X297mm) No. 83100644 Patent Application Revised Chinese Manual (δ August 5) A7 B7 V. Description of Invention () Printed by H- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] benzene Phenyl] -4- (benzylsulfonyl) -2-thiophenesulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2- Oxy-211-cyclooctyl [b] piperazine Uran-3-yl) methyl] phenyl] -5- (phenylsulfonyl) -2-thiophenesulfonamide H- [3- [cyclopropyl (5,6,7,8,9,10 -'Hexahydro-4-hydroxy-2-oxy-211 -cyclooctyl [b] piperan-3-yl) methyl] phenyl] "4, iodo-benzenesulfonamide 5-ammonia-H- [ 3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-keto-2H-cyclooctyl [b] piperan-3-yl) methylΓphenyl ] -2-thiophenesulfonamide 4.5-dichloro-11- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -2-thiophenesulfonamide 4.5-dibromo-H- [3- [cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy- 2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-thiapansulfonamide benzsulfonamide, 4-chloro 1 -[3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) propyl] benzene Group] -benzenesulfonamide * 4-cyano-} |-[3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2k-cyclo Octyl [b] piperan-3-yl) propyl] phenyl] -H- [3- [cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy -2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -4-ethyl-benzenesulfonamide H- [3- [cyclopropyl (5,6,7,8,9 , 10-hexahydro-4-hydroxy-2-oxy-2 [1- ring Octyl [b] piperan-3-yl) methyl] phenyl> 4- (phenylazo) -benzenesulfonamide (+)-1 [3- [cyclopropyl (5,6,7 , 8,9,10-hexahydro-4-hydroxy-2-oxy __- 81 -_ This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the notes on the back first Qin refilled this page) -Installation_, ιτ Department of Economics Central Standards Bureau Staff Consumer Cooperative Co., Ltd. Printed No. 83100644 Patent Application Manual Chinese Specification Correction Page (δδ, 1985) A7 B7 V. Description of Invention (P) -2H- Cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4-fluoro-benzenesulfonamide (-)-N- [3- [cyclopropyl (5,6,7,8,9 , 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-fluorobenzenesulfonamidoaminocarboxylic acid * [2- [[3- (R or S)-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctane [b] piperan-3 -Yl) methyl] phenyl] amino] imidazol-4-ylmethyl) -2-copperethyl]-, 1,1-dimethylethyl ester aminocarboxylic acid, [2-[[3- (R or S)-[f propyl (5, δ, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl Phenyl] phenyl] amino] -1- (S)-(1H-oxazol-4-ylmethylΓ-2-one ethyl ]-, 1,1-dimethylethyl ester N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- meridyl-2-oxy-2} 1-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -phenylethanesulfonamide H- [3- [cyclopropyl (5,6,7,8,9,10-hexa Hydrogen-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (3-isofluorazolyl) -2-thienylamine N -[3- [Cyclopropyl (5,6,7,8,9,10-hexaki-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Phenyl] -3-pyridinesulfonamide (+)-| {-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H -Cyclooctyl [b] piperazin-3-yl) methyl] phenyl] -8-quinolinesulfonamide (-)-^ [3- [cyclopropyl (5,6,7,8,9- , 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenylquinolinesulfonyl- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (2-pyridyl ） -2-thiophene sulfonate __- 82 -_ This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) (Please read the note of "Φ" before filling this page)-Packing _ Line Revised page of Chinese Specification for Patent Application No. 831 00644 (8 5 years) A7 B7 V. Description of the invention ((P |) amine H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 氧基- Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- (hydroxyamino) -benzenesulfonamide H- [3- [cyclopropyl (5,6,7,8,9 , 10-Hexahydro-4-meryl-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- (dimethylamino) -benzenesulfonium 3-Amino- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl] -benzenesulfonamide and H- [3- [cyclopropyl (5,6,7,8,9, 10- "hexahydro-4-hydroxy-2-oxy-2, cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4: (trifluoromethoxy) -benzenesulfonylm — — 4- (bromomethyl > -1 [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide 4-[[[3- [Cyclopropyl (5, 6, 7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] amino] sulfofluorenyl] benzidine (-)-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy-2H-cyclooctyl-3-yl) methyl] phenyl] -1-methyl-1H-imidazole-4-sulfonamide N- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4- -Yl-2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (phenylsulfonyl)-, (S) -2-thiophenesulfonamide H -[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Phenyl] -5-methyl-3-pyridinesulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 {1 -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- (hydroxyamino) benzenesulfenamide 3-[[[3- [cyclopropyl (5,6,7 , 8,9,10-hexahydro-4-hydroxy-2-oxy _________ — S3 — This paper size applies to China National Standard (CNS) A4 (210 > < 297 mm) Patent Application No. 83100644 Revised page of the Chinese manual for the case (August 85) A7 B7 V. Description of the invention (SV) Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs-2H-cyclooctyl [b] piperan-3-yl) methyl] benzene Methyl] amino] sulfofluorenyl] -benzoic acid methyl ester H-C3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-ring Octyl [b] piperan-3-yl) methyl] phenyl] -3-hydroxy-benzenesulfonamide benzsulfonamide, 4-cyano 4- [3- [1- (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) butyl] phenyl]-N- [3- [Cyclopropyl [3- (2-isothiazolidinyl) phenyl] methyl- (5,6,7, 8,9,10-hexahydro-4-hydroxy-S, S * -dioxo jfb ) Methyl] phenyl] -3-[(phenylpentyl) amino] -4-2H-cyclooctyl [b] piperan-2-_3-chloro-N- [3- [cyclopropyl (5,6,7,8, ϋΐ〇-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3-[(benzene Sulfofluorenyl) amino] -1 -propanesulfonamido N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211 -Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- [methanol] -benzenesulfonium H- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3-[(2-ethanol) amino] -benzenesulfonyl Amine, and N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl] -3-[(bis (2-ethanol) amino] -crysaminol K is the best compound of the present invention: -4-cyano-N- [3- [cyclopropyl (5,6,7 names, 9,10-hexahydro-4 -hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,1, 3-Benzothi beer-4-Lutenamine (Please read the notes on the back first, and then fill out this page). Paper size applies to Chinese National Standard (CNS) A4 specification (210X; 297 mm) No. 831 00644 Patent Application Revised Chinese Manual (August 85) A7 V. Description of Invention (Suppression) Staff of Central Bureau of Standards, Ministry of Economic Affairs Consumption cooperation Du printed (+)-4-chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (-)-4-chloro-H- [3- [cyclopropyl (5,6,7, δ, 9, 10-hexahydro-4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (+)-4-cyano- N- [3- [Cyclopropyl (5, 6, 7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl Phenyl] -benzenesulfonamide (-)-4-cyano-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxyoctyl [b] piperazin-3-yl) "methyl] phenyl] -benzenesulfonamide. N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxy-2-oxy-211-cyclooctyl-3-yl) methyl] phenyl] -1-methyl " "-( S) -l Η-imidazole-4-sulfonamido (+)- Ν-3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] Phenyl] -4-fluoro- Sulfonamide (-)-N-3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -4-fluoro-benzenesulfonylsulfenylcarboxylic acid, [2-[[3- (!? or 5)-[cyclopropyl (5, &, 7,8 , 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl> methyl] phenyl] butylamino-1- (S)-(1H- Imidazol-4-ylmethyl) -2-_ethyl]-, 1,1-dimethylethyl ester (+) 4- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -8-Bquinolinesulfonamide (-) H- [3 -[Cyclopropyl (5,6,7,8,9, -10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -8-quinolinesulfonamide H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) methyl] phenyl] -4- (hydroxyamino) -benzenesulfonate-85-This paper is in accordance with the Chinese National Standard (CNS) A4 specification (210 × 297 mm). Fill in again — the page of loading τγ line No. 831 00644 patent application is the Chinese manual amendment page (August 85) A7 B7 V. Description of invention (W) Staff Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Manufacture_limb 4-[[[3- [cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctane [b] piperan-3 -Yl) methyl] phenyl] amino] sulfofluorenyl] -benzylamine (-)-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4 -Hydroxy-2-oxy-2H-cyclooct-3-yl) methyl] phenyl] -bumethyl-1H-imidazole-4-sulfonamine-3 [[[3_ [cyclopropyl (5,6, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -benzoic acid , Methyl ester ...... benzylsulfonamide, 4-cyano-bu [3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperazine- 3-ij butyl] phenyl]-H- [3- [cyclopropyl [3- (2-isothiazolidinyl) phenyl] methyl- (5,6,7, 8,9,10-hexahydro-4-hydroxy-S, S'-dioxide) methyl] phenyl] -3-[(phenylsulfonyl) amino] -4-2H-cyclooctyl [ b] piperan-2-_3-chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -3-[(phenylsulfonyl) fluorenyl] -1-propanesulfonamide N- [3- [cyclopropyl (5,6 , 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 {{-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- [methanol]- Besysulfame N-C3- [ring (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-211-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- [ (Bis- (2-ethanol)) amino] -benzenesulfamethoxamine-Description of preferred specific spring examples • Prepared under K and examples and in the full text of this document: The spoon is the number of degrees Celsius (please read the note on the back first # fc-装 —Fill in this book again and again ¥ ο Thread ______- 8 8 A paper size applies to the Chinese national standard (CMS> Α4 specification (210X297 mm) ϋ Η 4 ί i} \ A6 B6 V. Description of the invention (85 ) Μ is Moore (Mae degrees) Η is equivalent (concentration) n L is 奄 Lig og is «gram nnHg is millimeter column is 霣 NMR spectrum 13C-HMR is carbon nuclear magnetic resonance spectrum δ is a chemical relative to TMS Displacement (parts per million) CDCls are secondary gas imitation CDaOD is secondary formazan DHSO is secondary dimethyl sulfide FAB MS is fast atomic strike volume light 谮 El MS is the best quality of 轚 衡 衡 质 HRMS It is a high-resolution fluorescein spectrum Anal is an analysis data Pd / C is palladium / inflammation THF is a tetrakistrifurethane and the following examples illustrate the present invention: Preparation of 1 2- (4-phenylbutyryl Salicylic acid ethyl ester (formula A-2), see circle A. 1.00 g of 4-benzylbutyric acid and 60 g of H, M-dimethylaminobenzyl; in a 20 ml solution of dichloromethane, add 0.7 5¾ liters of ethyl salicylate and 0.95 ml of diisopropylcarbodiimide. After 18 hours * the mixture was decompressed and shrunk. The residue was ground from ethyl acetate. The organic calendar was washed with an aqueous solution of sodium argon carbonate and water, dried (magnesium tellurate), and shrunk under reduced pressure. K10% ethyl acetate / -87-

This paper uses national standard (CNS) A4 specifications (210X297)

I Printed by the Central Bureau of Standards and Quarantine of the Ministry of Economic Affairs, Shellfish Consumer Cooperative, A6 B6 _______ —---- ----------------- V. Description of Invention (86) Fast upward chromatography on the stone · It can produce 1.61 grams of the title product as a colorless oil. The physical properties are as follows: aH HHR δ 1.32; 2.10; 2.65; 2.76; 4.28; 7.06; 7.25; 7.5; 8.01 »

Example Γ 4-Hydroxy-3-phenylethyl # fantin [Formula A-3 > (In a flame-flammed flask), add 94 «solution of 儋 1 to 2.0 奄 liter of benzene. The mixture was heated overnight at 80 ° C *, then cooled and the formazan was discontinued. The astringent is divided into diethyl ether and 1H «sodium oxide, and then the ether is washed twice with ether. Acidified water calendar produces white precipitate * is M4 parts of dichloromethane-formaldehyde extraction. The organic layer was reduced and the residue was reduced to SiO 50-70 ¾ ethyl acetate / hexane on silica, which could produce 16 mg of white solid title product. The physical properties are as follows: XH NMR δ 2.87; 3,33; 7.25; 7.51; 7.86〇13C HMR δ 25.54; 33.62; 104.54; 115.99; 116.25; 122.75; 123.54; Γ 25.48; 127.85; 128.10; 131.08; 141.41; 151.94; 160.85; 164.

El HRMS [·] = 266.0936 〇

Preparation 2 2- (5-Bentylpentyl) hydrosulfate ethyl (Formula A-4) See 鼷 A for 1.07 g of 5-phenylvaleric acid and 60 奄 g of U, Η-dimethylaminopyridine at 20 To a milliliter of the methylene chloride solution, 0.75 liters of acetic acid salicylate and 0,95 liters of diisopropylcarbodiimide were added. After 18 hours, the mixture is decompressed -88- This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) (Please read the precautions on the back before filling this page)-#:-装 第 831 00644 No. Patent Application Revised Chinese Specification Sheet (August 1985) A7 B7 V. Description of the Invention (Magic 7) Concentrated, and the residue M ground with ether. The organic layer was washed with aqueous sodium bicarbonate solution, dried (magnesium acetate), and concentrated under reduced pressure. Flash chromatography on M 10% ethyl acetate / hexane gave 1.60 g of the title product as a colorless oil. The physical properties are as follows: AH NMR δ 1.31; 1.75; 2.65; 4.25; 7.04; 7.2; 7.49; 7.99 ° IR 2937, 1765, 1723, 1294, 1272, 1261, 1204, 1133, 1121, 1082 cm-1. ”-Analytical measured values: C, 73.37; Η, 6.72. Example 2 4-Hydroxy-3- (3-phenylpropyl) tilitin (formula A-5) is shown in Figure A. To a suspension of 80 mg of 60% sodium hydride / mineral oil in 3.0 ml of benzene in a flame-drying flask was added 326 mg of a solution of the preparation 2 ester in 60 ml of benzene under argon. The mixture was refluxed overnight, cooled again and quenched with methanol. The mixture was partitioned between acetic acid and 1N sodium hydroxide, and the aqueous layer was washed with 2 parts of ether. The aqueous layer was acidified to form a precipitate, which was extracted with K4 parts of dichloromethane-methyl ether. The organic layer was condensed under reduced pressure and flash-chromatographed on silica with 50-70% ethyl acetate / hexane to give 108 mg of the title product as a white solid. The physical characteristics are as follows: Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 隠 5 1.87; 2.63; 2.72; 7.2; 7.49; 7.87 ° 13C HHR δ 23.35, 29.46, 35.41, 104.94, 116.09, 116.16, 122.81, 123.51, 125.45, 128.02, 128.21, 131.06, 142.11, 151.97, 160.J3, 164.55 °

El HRMS [m] = 280.1102. Preparation 3 Ethylenediamine-Diacetic acid ______-S 9 -______ This paper rule applies to China National Standards (CNS) Standard 4 Recruitment Plant (21 × 297 mm) Member of the Central Standard of the Ministry of Economic Affairs X. Consumer Cooperatives Preparation of A6 B6 V. Description of the invention (88 pairs of 0.67 g of ethylenediamine in 5 l of cold (01c :) stirred ether solution, dropwise added 1.3 ml of a solution of acetic acid in 5 l of ethyl acetate. The mixture was thickened by sinking forgings, simmered for 5 minutes in the chamber, and then mixed with coarse glass to meet the «. The solid was thoroughly washed with ether. Then dried to constant weight in the air, 1.68 grams of white The titled product of solid 笾. The physical properties are as follows: Mp 115-116.5t: (see Fieser & Pieser »〇1 13, value of ρ · 172 >.

Preparation 4 2-naphthyl dimerization ((Formula B-3, where R is fluoren-2-yl)) See B. 778 g of 4-hydroxypanrulin of formula B-1, 312 mg of formula B-2 2-naphthaldehyde, in which R is naphthalen-2-yl, and 18 g of EDDA (in 8 ml of absolute acetic acid) were sown overnight. The precipitated solid M intermediate glass frit was filtered * washed once with cold ether and dried under vacuum to give 722 g of the title product as a pale yellow solid. Preparation 5 Dibenzylmethyl dimer (Formula B-3; where R is dibenzylmethyl) see β diagram for 1.56 g of formula B-1 4-hydroxycoumarin * 0.71 liter formula B- 2 phenylacetaldehyde, in which R is dibenzylmethyl * and 36 奄 g of EDDA in 16¾ liters of absolute acetic acid, sowing at room temperature for 7 days. The precipitated solid M is filtered through a medium-sized glass frit. However, the separation, washing with cold ethyl acetate twice, and drying under vacuum can produce 945 g of the title product, which is a white solid. The physical properties are as follows: FAB HRMS [η + Η] = 503.1511. Preparation 6 Phenyl Methyl dimer (Formula B-3; where R is <-methylbenzyl 90

”A ice * NS value 〖nNS) review 4 枧 蝽 (210 乂 297 public power) A6 B6 5. Description of the invention (of)

&gt; See picture B. 778 g of 4-hydroxycoumarin of formula B-1, 0.27 ml of 2-benzylpropanal of formula B-2 (wherein 11 is "-methylbenzyl), and 18 mg of EDDA In 3 ml of a mixture of ethanol and ethanol, stir at room temperature. Precipitated solids are separated by filtration through a medium-grade glass frit. M is washed with cold ethyl acetate, and then dried under vacuum until 268 mg of the title compound is formed. The physical characteristics are as follows:

Rr = 0.43 (EtOAc) 〇 FAB MS [B + m = 441 »Example 3 4-Hydroxy-3- (2-naphthylmethyl) coumarin (Formula 8-43) See 鼷 8 440 mg Preparation 4 祢 踵A mixture of the product and 120 mg of sodium cyanocyanide in 15¾ liters of formic acid was flowed under nitrogen for 2 days, after which TLC showed that some of the starting material remained. Add additional sodium cyanohydrin (100 mg) and continue to flow for another day. The formazan was removed under a stream of nitrogen, and an aqueous ammonium hydroxide solution was added, and the mixture was passed through the mixture. The solid M was washed thoroughly with water and dried under vacuum. K produced 267 g of the standard product as a white solid. The physical properties are as follows: aH MMR (d-6 DHS0) δ 3.82: 7.0-7.9〇13C: δ 31.09, 97.66. 116.35, 122.52, 124.08, 125.33, 125. 42. 126.33, 126.41, 127.71, 128.04, 128.17, 129. 16, 130.27, 132.22, 133.99, 142.85, 154.44, 165, 63, 172.52 〇 FAB MS [a + H] = 303.1015 ° Example 4 4-hydroxy- 3- (2,2-diphenylethyl)- Coumarin (Form B-4b) see -91- This paper size is applicable to China National Standard (CNS) A4 specification (21 × 297 mm) (谙 Please read the precautions on the back before filling in this page &gt; . Printed by A6 B6 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of Invention (9)

Drawing B: 640 mg was prepared as a mixture of the product 5 and 240 g of cyanocyanine in 19 L of formic acid, heated under argon. Gangue flow for several days * Regularly add about 2500 g of sodium cyanoborohydride. The mixture was subdivided into ethyl acetate and an aqueous ammonium hydroxide solution, and the organic sulfonium (magnesium sulfate) was dried and sprayed to form a solid with extremely poor solubility. This is most likely to be dissolved in chloroformase and adsorbed on silica using 20% ethyl acetate / digas methane chromatographic flash chromatography. The product fraction is believed to produce 335 g of the product as a white solid. The physical properties are as follows: Μ.ρ. 233-234.5t :. XH NMR (d6-DMS0) 8 3.29; 4.48; 7.1-7.3; 7.42; 7.67

El MS [β] = 342. Example 5 4-Hydroxy-3- (2-benzylpropyl) myristotin (Formula B-4c) is shown in Figure B. 157 g of 6 g of the product and 45 g of sodium cyanohydrolanine were prepared in 5 ml. Mix the formazan with argon for 2 days * and add 1 part of 60mg of kangin agent in the middle. Formazan removed: The mixture was partitioned between ethyl acetate and an aqueous ammonium solution. Wash the calendar with water, dry it (magnesium sulfate), and concentrate under reduced pressure. Rapid analysis of Ml: l ethyl acetate / hexane on silica produces 87.5 g of the title product as a white crystalline solid. The physical properties are as follows: _

Rf = 0.35 (1: 1 ethyl acetate-hexane)-M.p. 15 8-15 9 t: -92- This paper size is in accordance with China National Standard (CNS) A4 specification (210X297 mm) .. ...-.......................................-... ............................................... Order. ....... (Please read the notes on the back before filling this page)

Central Bureau of Standards, Ministry of Economic Affairs, Shellfish Consumer Cooperation, A6 __B6 _ V. Description of Invention (91) 'H HHR 5 1.41; 2.78; 3.02; 3.16; 7.2; 7.50; 7.75 FAB HRMS [a + h] = 281.1170 Preparation 7. Formamidine 3,3-diphenylpropionate (H-methoxy)

C 1. 13 g of diphenylpropionic acid and 537 g of hydrazone, 0-dimethylhydroxylamine, acid salt, in 10 ml of dichloromethane cold (0 &quot; C &gt;) suspension, add 28 l of diisopropyl Amine (most solids will dissolve) · Add 1.27 grams of bis (2-oxy-3-0? Azolidinyl) phosphine sulfonium chloride. Stir the solution at 0 t: Add it to the chamber. Gently stir the solution. The solution was washed with a large amount of dilute hydrochloric acid, and extracted with two portions of dichloromethane. The mixture was dried organically (magnesium sulfate) and concentrated under reduced pressure. The residue was placed on silica κ 40- Fast decantation with 50% ethyl acetate / hexane gave 1.31 g of the title product as a colorless oil. Physical properties are as follows: = 0.35 (1: 1 ethyl acetate-hexane> ^ NMR 8 3.09; 3.18; 3.55; 4.69; 7.2-7.3 IR 3027, 2937, 1661, 1495, 1450, 1417, 1385, 994, 752, 739, 7 &lt;? 1 cm-i.

El MS [m] = 269 Analysis found: C, 75.10;., 7.17; 5.12 Preparation 8 3,3-Dibenzylpropionaldehyde (formula (: -3) see circle 0 for 1.26 grams of preparation 7 In 19 liters of cold tetrahydrofuran (0t: &gt;) stirring solution, 213 g of lithium aluminum hydride was added in M-times. After 45 minutes at 01C, the dark gray slurry was sucked into ice and 25 ml of 1M hydrogen sulfate. Potassium-93- 乂 Paper Size 逋 National Standard (CNS) A4 Specification (210X297mm) {Please read the precautions on the back before filling this page)-Binding, A6 B6 Central Standard of the Ministry of Economic Affairs Printed by the Bureau ’s Consumer Cooperatives. 5. Description of the invention (92) in the slurry. The mixture «filtered to remove a small amount of insoluble inorganic matter, and the organic phase was extracted with another portion of ether. ) And concentrated under reduced pressure to produce 980 g of the title product as a colorless oil. The material thus obtained can be used without purification. The physical properties are as follows: RfO. 34 (20% ethyl acetate / hexane) MMR δ 3.17; 4.64; 7.1-7.4 ί 9.74 Preparation of 9 2-phenylbutyric acid methyl (K-methoxy) amidamine (formula C-5) See Figure C for 1.64 g of 2-phenyl Acid and 976 g of Ν, Ο-dimethylhydroxylamine hydrochloride in 20 ml of dichloromethane in ice-cold (0Ϊ :) soaking suspension • Add 5.6 奄 liters of diisopropylethylamine (most solids will dissolve ), And then add 2.55 grams of bis (2-oxy-3-blazolidinyl) phosphine gas. Stir the solution for 0.5 hours under Ot: * Allow to warm to room temperature and stir overnight. The solvent is then moved under a nitrogen stream. • The residue was partitioned into ethyl acetate and water containing 12 liters of 1H hydrochloric acid. The aqueous phase was diluted with a dilute aqueous solution of sodium bicarbonate and brine, dried (magnesium sulfate), and then decompressed under reduced pressure. The residue was on silica. Rapid decantation with 35% ethyl acetate / hexane * can produce 2.06 g of the title product as a colorless liquid. The physical properties are as follows: Rf = 0.30 (30% Z * acetate / hexane) aH HHR δ 0.87; 1.7 ; 2.1; 3.15; 3.47; 3.89; 7.3, IR 2967, 1662, 1461, _1454, 1382, 997, 700 cm 〇 El MS [β] = 20% (Please read the precautions on the back before filling in this page) # -Loading; τ -94--This paper size is applicable to Laos. National Sample Standard (CNS) A.4 Specification (210x297 mm) No. 83100644 Patent Application Chinese Specification Correction Page August 1985) A7 __B7 V. Description of the invention Preparation of 10 2-phenylbutyraldehyde (Formula C-6) See Figure C. For 1.45 g of Preparation 9 of the title product in 28 ml of anhydrous tetrahydrofuran, cooled under argon (0¾) Mix the solution and add 3 to 50 mg of lithium aluminum hydride. After 45 minutes at .0¾, the dark gray slurry was sucked into ice and 35 ml of a stirred slurry of 1M potassium hydrogen sulfate. The mixture was decanted to remove a small amount of insoluble inorganic 'organic phase and extracted with another portion of ether. The combined organic phases were washed with brine, dried (magnesium sulfate), and concentrated under reduced pressure to give 1.06 g of the title product as a colorless oil. No further passivation is required after the substance is obtained. The physical properties are as follows: = 0.46 (20% ethyl acetate / hexane ^ &quot; H NMR δ 0.90; 1.8; 2.1; 3.4; 7.3 Example 6 4-hydroxy-3-U-methylbenzyl) -coumarin ( Formula D-3, where

R is ct-methylbenzyl) See Figure D. 500 mg of 4-hydroxycoumarin of formula D-1 was printed in 2.8 ml of U-bromoethyl of formula D-2 by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs.)- A suspension of benzene (wherein R is α-methylbenzyl) was heated to 155T at room temperature for 0.5 hours. After 0.5 hours at 1551C, 4-hydroxycoumarin was dissolved and a dark orange solution was formed. After a total of 2 hours at 155¾ * the solution was cooled to room temperature (the reaction mixture solidified). The material was distributed between 10 ml of diethyl ether and 25 ml of 1N sodium hydroxide. The aqueous layer was washed with K diethyl ether, and K 6N hydrochloric acid was acidified to pH = 1; the resulting precipitate, M dichloromethane / formamidine, was repeatedly extracted. The combined organic extracts were dried (magnesium sulfate) and concentrated under reduced pressure. The residue, K 50% to 70% ethyl acetate / hexane, was subjected to fast-pass column chromatography to give 430 mg of the title product as a white solid. The physical characteristics are as follows:-___- 95-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) V. Description of the invention (94) A6 B6 HMR 8 7.84, 7.45, 7.3-7.2, 4.65, 1.71; IR (Reconciliation &gt; 3237, 2925, 1671, 1627, 1396, 752 cm ^ Printed by EI-MS M + = 266.0946 (measured value) printed by the Central Laboratories of the Ministry of Economic Affairs, Monthly Industrial Cooperative) Example 7 4-hydroxy-3-diphenyl Methyl coumarin 324 g of 4-S coumarin and 368 g of commercially available diphenyl formamate, 30 liters of dibenzane mixture. Add trifluoride trimethyl ether acid. Hydrocarbon chamber After 100 hours at room temperature, the reaction solution M was diluted with 40 ml of diethyl ether and washed with water. The dried solution was dried (magnesium sulfate) and the pressure was reduced. The residue was 20% to 80 涔 Z> ethyl acetate / hexane. Column chromatography can produce 587 mg of organic thin product. The physical properties are as follows: 1 HMR δ 7,73, 7.55, 7.42-7.23, 6.25, 5.99; FAB-MS [· + Η] = 329 (Actual value &gt; Example 8 4-Hydroxy-3- (3-hydroxy-1-phenylbutyl) -coumarin to 924 mg of a milky white suspension of warfarin in diethyl ether • In Ot: and argon Slowly add (batch) 12 5¾ grams of lithium hydride anchor to the gas. Hydrocarbon Ot: After 3 hours, the reaction is warmed to room temperature. After 1 hour, the mixture is cooled to 0D, and 5 ml of water and then 10 liters of 1 Η 氡 sodium oxide slowly treatment. Once the effervescence is stopped, the tiller is washed and the water calendar is washed with diethyl ether * Μ 6Ν hydrochloric acid is acidified, and repeated extraction with dichloromethane (formaldehyde-chloroform as a latent solvent) .Mixed with dry calendar (_magnesium sulfate) and decompression thickener. Residue M 2% to 20% formazan / dichloromethane flash column chromatography 'can produce 590 g of the title product Enantioisomeric mixtures * are white solids. -96- This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) (谙 Please read the precautions on the back before filling this page) _ #.-装· Printed by A6 _B6_ of the Consumer Cooperatives of the Central Bureau of Standards and Happiness of the Ministry of Economic Affairs 5. Description of the Invention (叼) The physical characteristics are as follows: HHR 3 7.91, 7.48-7.15, 4.59, 3.76, 2.59, 2.06, 1.25; Ι1Ϊ (谞 和 的) 3294, 2924, 1677, 1611, 1495, 750 cm-1 EI-MS M + = 310 (measured value) Preparation of 11 1-bromo-2-methyl-1-phenyl Alkane (Formula D-2: where R is 2-methyl-1'phenylpropyl) See HD In a flame-dried flask equipped with a reflux condenser, add 3.0 grams of commercially available 2-formaldehyde in an argon atmosphere Propyl-1-phenylpropan-propionate. Fermentation M 0.60 liters Tribromo M dropwise slow processing. Once added * the exothermic mixture is refilled and becomes biphasic. After 0.25 hours, the reaction was divided into diethyl ether-hexane and water. There is a dilute aqueous solution of ammonium carbonate, washed with water, dried (magnesium sulfate) and concentrated under reduced pressure. Using a cooling bath, 4.44 g of crude title compound is obtained. • It is a clear, colorless oil. The crude bromide can be used directly in the next reaction without further purification. The physical properties are as follows: 1 NMR S 7.25 · 13. 19, 1. 4 Example 9 4-Hydroxy-3- (2-methyl-phenylphenylpropyl) -coumarin (Formula D-3: where R is 2-methyl-phenylphenylpropyl) 2 In a pressure tube of 50 mg 4-hydroxymyristotin, 2.14 g of crude bromo-2-methyl-l-benzylpropane from Preparation 11 was added. The resulting suspension was tightly sealed and heated to 110: 2. After an hour, the mixture was heated to 150 ×: one night. The resulting red solution was cooled to room temperature, and distributed between diethyl chain and -97- This paper uses national standard (CNS) A4 specifications (210x297 mm) (Please read the notes on the back before filling in this page)

Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 B6 V. Description of the invention (96) 1N argon oxidation chamber. The aqueous layer was washed with M diethyl ether and acidified with M 6HSI to cH = 1, and then repeatedly extracted with dichloromethane (formaldehyde-chloroform latent solvent). The combined dichloromethane extract was dried (magnesium sulfate) and concentrated under reduced pressure. Residual seedlings were decanted using 30% to 50% ethyl acetate / hexane in a rapid column to produce 148 g of the titled product as a black solid. The physical properties are as follows: NMR δ 7.84, 7.59, 7.42, 7.31-7.13, 3.99, 3.14, 0.97, 0.90; IR (harmonic) 3254, 2925, 1655, 1616 · 754 cm-1; EI-MS M + = 294. 1249 (Measured value). Make a solution of 12 phenyl-1-butyrate to 890 g of commercial phenylbenzyl pyridine in 30 ml of diethyl ether. Mix the solution with 250 g of lithium aluminum hydride and add it in portions. . After 2 hours, the gray solution M was treated slowly with 0.25 ml of water and then 1.10 L of 1N sodium hydroxide. After 0.5 hours * the pre-formed precipitate was filtered through a magnesium sulfate plate, and diethyl ether was used as a lotion. The mash is shrunk under reduced pressure. It produces 0.90 g of clear titled product as a colorless oil. This product was used directly in the next reaction without further purification. 'The physical properties are as follows: 1 NMR 5 7.27, 4.61 and 4.59, 2.27, 1.77-1.57, 1.4 and 1.22, 0.90. Example 10 4-Hydroxy-3- (bufenamyl butyl) -myristotin was prepared from 792 g of 4-hydroxycoumarin and 809 g of 12 phenyl-1-butyrate in 25 ml Mixture of alkane * Add 2.6m-98 in argon atmosphere- This paper size is in accordance with Chinese National Standard (CNS) A4 specification (210 乂 297mm)

{Please read the notes on the back before filling in this page J

A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (9 * 7) Lithium tribasic phosphonate. The resulting yellow solution was allowed to stir overnight at room temperature. The volatiles were removed and the residue was partitioned between diethyl ether and 1K sodium hydroxide. It was washed with K-diethyl ether and then acidified with 6 M hydrochloric acid to give = 1. The resulting precipitate was repeatedly extracted with dichloromethane (formazan-aqueous imitation). Mix @ 二 《Methane extract, K, dilute sodium bicarbonate, wash once, remove most of the unreacted 4-hydroxymyristotin, wash again with water, dry (magnesium sulfate), and finally under dysentery concentrate. The residue was adsorbed to the gravel, and 40% to 50% ethyl acetate / hexane was used to perform a fast column analysis * to produce 183 grams of the titled product, as white crystals. The physical properties are as follows: 1 NMR δ 7.84, 7.47, 7.33-7.17, 4.51 and 4.48, 2.40-2.27, 2.21-2.09, 1.37, 0.95; IR (harmonic) 3192, 2926, 1674. 1669, 1604, 1202 cm, EI- MS M + = 284.1259 (found). Preparation 13 Stirred suspension of 1-phenyl-1-pentanylpyrazole 1.20 g of lithium aluminum hydride in 100 liters of diethyl ether * Under otto and argon atmosphere, slowly add 4.'40 liters of commercial propylene A solution of phenylphenylhydrazone in 5.0 ml of diethyl ether over 10 minutes. After 0.5 hours, the gray suspension was warmed to room temperature. After 1 hour, the reaction mixture was cooled down again to 0 t: • and 2.5 ml of water, and then treated with 5.50 ml of 1H sodium hydroxide. After 1 hour, the white precipitate formed was filtered through a magnesium sulfate pan, and M diethyl ether was used as a lotion. Maize shop can produce 4.5 g of phenyl-1-pentyl ferment as a clear, colorless oil under the reduced liquid. This product can be directly used in the next reaction without further advancement (please read the precautions on the back before filling in this page) -99- This paper size adopts China National Standard (CNS) A4 specification (21 〇χ297mm) A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (98)-one step purification. The physical properties are as follows: 'H NMR δ 7.31, 4.65, 1.95, 1.82-1.68, 1.40-1, IS, 0.87 〇 Example 11 4-hydroxy-3- (1-phenylpentyl) -myristotin pair contains δΐΐ 奄G of 4-hydroxycoumarin and 985 g of ketophenyl-1-pentanase in a flame-dried flask of a mixture of 30 ml of dioxane * 30 ml of boron trifluoride etherate was added under argon. The resulting yellow solution was allowed to sow at room temperature overnight. The volatiles were removed and the residue was partitioned between diethyl 81 and 1N sodium hydroxide. The test leeches were washed with diethyl ether and then acidified with 6N hydrochloric acid to give = 1. The resulting precipitate was repeatedly extracted with dichloromethane (formaldehyde-nitroformate as a latent solvent). The mixed dichloromethane extract was diluted with sodium bicarbonate once to remove most of the unreacted 4-hydroxycoumarin, washed with brine, dried (magnesium sulfate), and finally concentrated under reduced pressure. . The residue was adsorbed onto silica and 40% to 50% ethyl acetate / hexanes were subjected to flash column chromatography * to yield 193 mg of the title product as white crystals. The physical properties are as follows: 'aH NHR δ 7.87, 7.48, 7.29-7.17, 4.65, 2.43-2.31, 2.23-2.14, 1.43-1.24, 0.87; IR (Rhowa) 3223, 2925. 1676, 1669, 1605, 1196 cm ^ EI-MS Μ + = 308 · 1423 (actual sea value); found by elemental analysis: C, 77.52, thallium, 6.66. Preparation of 14 1- (4-bromobenzyl) -2-methylpropane -1-Ferment &lt; Please read the notes on the back before filling in this page} -Binding. &Quot; -100- This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm) Ministry of Economy 4-central standard A6 B6 printed by the Bureau Cooperative Consumer Cooperative. V. Description of the invention (99) To the flame-dried flask * 1.85 grams of commercial 4-O-benzaldehyde and 30 liters of tetrahydrofuran were added under argon. The solution was cooled to , And then 7.0 M liters of isopropylmagnesium bromide slowly treatment. After stirring overnight at room temperature • The reaction mixture was concentrated under reduced pressure. The residue was partitioned between diethyl ether and ammonium chloride, water The layers were extracted with dimethyl ether. The mixed organic calendar (magnesium acetate) was removed. The volatiles were removed. The residue was analyzed by 30% to 60% diethyl ether / hexane in a fast column. Μ was 1.25. Hurricane products • It is a thick brown oil. The physical properties are as follows: 'H NMR δ 7.42, 7.13, 4.28, 2.27, 1.86, 0.94, 0.76 〇 Example 12 3- (1- (4-bromobenzyl) -2-methylpropyl) 4-Hydroxycoumarin is suspected of containing 1- (4-bromophenyl) -2-methylpropan-propionate of 14 in 324 mg of 4-hydroxypumarol and 573 g of dioxane In a flame near-solution dry flask, 1.2 ml of trifluoride etherate was added under argon atmosphere. The resulting yellow solution was stirred overnight at room temperature. The volatile matter was removed and the residue was partitioned between diethyl ether and 1N hydrogen. Sodium oxide. Washed with M diethyl ether and acidified with M 6N hydrochloric acid to give out = 1. The resulting precipitate M was re-extracted with methanol (methanol-aqueous imitation as a latent solvent) and repeatedly extracted. The mixed methane The extract was diluted with sodium bicarbonate once to remove most of the unreacted 4-hydroxycoumarin, and then washed with brine, dried (magnesium sulfate), and finally concentrated under reduced pressure. The residue was adsorbed to silica And flash column chromatography · K 50% to 60% acetic acid / hexane, M to produce 28 奄 Beijing title product, a brown solid. The physical properties are as follows: HHR δ 7.86, 7.50- 7.44, 7.35, 7.25, 3.94, -101- This paper size adopts China National Standard (CNS) A4 specification (210X297 mm) (谙 Please read the precautions on the back before filling this page). Order. A6 B6 printed by Shelley Consumer Cooperative of the Standards Bureau. 5. Description of the invention (100) 3.10, 0.95, 0.88; EI-MS M + = 374 and 372 (measured values). Prepare 15 1,2-dibenzyl acetic acid, 1.20 g of lithium hydride in 100 ml of diethyl ether, and slowly add 5.50 g of commercialized deoxybenzene to the atmosphere at 0 ° C and in the atmosphere. 25.0 liters of diethyl ether solution. After 0.5 hours, the gray suspension was warmed to room temperature. After 1 hour * the reaction mixture was cooled to 0 ° C again: 1.25 ml of water and 5.50 liters 1 Η sodium hydroxide and treated afterwards. After 0.5 hours, the resulting white precipitate was filtered through a magnesium sulfate disk, and the diethyl ether was washed. The mash is shrunk under reduced pressure to produce 5.50 g of osmium product * as white crystal osmium. This product can be used directly in the next reaction without purification. The physical properties are as follows: 1 NMR δ 7.38-7.12, 4.80 and 4.78. 2.95, 2.17. Example 13 3- (1,2-dibenzylethyl) -4-hydroxymyristotin pair contains 810 mg of 4-hydroxymyristole And 1.20 mg of 1,2-dibenzyl acetic acid preparation 15. In a 30 ml flame-dried flask of dibenzyl depleted solution, 3.0 liters of boron trifluoride etherate was added under an argon atmosphere. The resulting yellow solution should be stirred at room temperature overnight for an additional 48 hours. V ‘· r The hair substance is removed * and the residue is divided between diethyl ether and sodium hydroxide. The alkaline water was washed with diethyl ether * and acidified with M 6K acetic acid to out = 1. The produced effluent, M2 gas methane, is extracted (repeatedly) (M formase-aqueous imitation is a latent solvent). The mixed dicyanomethane extract M diluted with carbonic acid was washed to remove most of the unreacted 4-hydroxycoumarin · water solution, dried can (magnesium sulfate) and finally sickle under pressure. Residue is adsorbed to silica, and 40% to 50% -102- The size of this air bar is applicable to China National Standard (CNS) A4 specification (210X297 mm) (Please read the precautions on the back before filling this page}. Binding: ¥ A6 ___ B6 __ 5. Description of the invention (101) Acetylacetate / hexane was subjected to flash column chromatography, and M produced 167 mg of the title product. It was a white solid. The physical properties are as follows: M MMR δ 7.77 · 7.55, 7.36, 7.29-7.06, 4.88 and 4.85, 3.80 and 3.74, 3.48 and 3.42; IR (thickness) 3172, 2924, 1668, 1607, 1170, 699 cm 1 Preparation of 16 3-methyl-1-benzene In a flame-dried flask under an argon atmosphere, ketidine-bufer was charged with 0.50 ml of isoprene and 15 liters of diethyl ether. The solution was cooled to Ot: 2.0 M liter (3.0 M in diethyl ether). ) Treated with phenylmagnesium bromide. The mixture was warmed to room temperature overnight and then partitioned into diethyl ether and saturated ammonium chloride. Hydrogenated diethyl chain extraction> and mixed with calendar Dry can (magnesium sulfate), and finally reduced pressure and shrinkage. The residue M 20% diethyl ether / hexane was subjected to flash column chromatography to produce the title product in the form of g. The physical properties are as follows: aH NMR δ 7.30-7.10, 4.60, 2.84, 1.69-1.55, 1.47-1.40, 1.28, 0.90, 0.87 »Example 14 4-hydroxy-3- (3-methyl-1-phenylbutylbenzene Printed by the Consumer Cooperative of the Central Standards Bureau of the Coumarin Ministry of Economy {Please read the precautions on the back before filling this page}. Pack ¥ For 3-methyl 3-methyl 16 containing 650 mg of 4-hydroxypumarol and 800 mg -1-Bentyl butanol was burned in a dry flask of 25 liters of dioxane near solution flame. • 2.5_ liter of trifluoride sulfonium etherate was added in an argon atmosphere. The resulting yellow solution made it Stir under room temperature. After 3 days * the volatile matter is removed and the residue is partitioned between diethyl ether and 1N sodium hydroxide. Aqueous aqueous layer K diethyl ether_103_ This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) A6 ____B6_ V. Description of the invention U〇2) Washing and acidification to M 6Η »acidified to = 1. The resulting precipitate« M diazenium methane repeated extraction (formase-chloroform 漘 solvent). Mixed Dichloromethane extract κ dilute argon carbonate to remove most of the unreacted 4-hydroxycoumarin once, then rinse with brine, dry (magnesium sulfate), It was then concentrated under reduced pressure. The residue was adsorbed to silica * and K 30¾ to 40% ethyl acetate / hexane was subjected to rapid column analysis. K produced 248 g of the title substance as a white solid. The physical properties are as follows: NMR δ 7.85, 7.52-7.43, 7.31-7.17, 4.62, 2.41 -2.31, 2.20-1.90, 1.60-1.51, 0.96: IR (reconciled) 3221, 2925, 1670, 1624, 1397 · 750 cm, EI-MS M + = 308 (Measured value). Elemental analysis found: C, 77.82, H, 6,52. Example 15 3- (Cyclopropylphenylmethyl) -4-hydroxycoumarin (Formula D-3; printed by Shelley Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs (please read the precautions on the back before filling the nest) Page). Packing ¥ in which R is cyclopropylphenylmethyl) See Figure D. Contains 650 mg of 4-hydroxycoumarin of formula D-5 and 741 mg of formula D-4 ot-amylpropylbenzylase. R is cyclopropylphenylmethyl. In a dry flask of 20 ml of dioxane mixture, add 2,5 ml of boron trifluoride etherate under argon atmosphere. The resulting yellow solution was allowed to stir at room temperature. After 3 days, the volatiles were removed under reduced pressure, and the residue was partitioned between diethyl ether and 1 Torr sodium hydroxide. The basic aqueous layer was washed with M diethyl ether and acidified with M 6N hydrochloric acid to give = 1. The resulting precipitate was repeatedly extracted with dichloromethane (methanol-chloroform as a latent solvent). The mixed dichloromethane extract was washed with sodium bicarbonate once, removed most of the unreacted 4-hydroxymyristotin, and washed with water-104- &lt;: This paper size is applicable to Chinese national standards ( CNS) A4 specification (210x297 mm) A6 printed by Bei Gong Xiao T Cooperative, Central Standards Bureau of the Ministry of Economic Affairs ___B6_ 5. Description of the invention (103), dry suspect (magnesium sulfate), and finally concentrated under reduced pressure. The residue was adsorbed on silica and subjected to flash column chromatography with 40% to 60% ethyl acetate / hexane to produce 580 mg of the title product as a white solid. The physical properties are as follows: 'H NMR δ 7.87, 7.52, 7.32-7.20, 3.75, 1.90-1.81, 0.81-0.74, 0.57-0.52, 0.41-0.31; IR (reconciled) 2925, 1671. 1662, 1604, 1560 · 761 cm -1; EI-MS M + = 292 (found). Preparation 17 1,3-diphenylpropan-2-enzyme 1.10 g of lithium aluminum hydride in 50 ¾ liter of diethyl ether soaking solution • Under 0 ΐ: in an argon atmosphere * 鑀 slowly add 5.3 0 grams of commercialization 1 , 3-Dibenzylpropanidine in 10.0 liters of diethyl ether. After 0.25 hours, the gray suspension was warmed to room temperature. After 1.5 hours, the reaction mixture was cooled again to Ot: and slowly treated with 1.2 mL of water and 5.0 mL of IN sodium hydroxide. The white precipitate formed after 1 hour was filtered through a magnesium sulfate plate, and K diethyl ether was used as a lotion. Concentrate M under reduced pressure to produce 5.2 g of standard product, which is a viscous, clear and colorless oil. This product f was used directly in the next reaction and repurified. The physical properties are as follows: aH NMR δ 7; 35-7.20, 4.05, 2.8, 1.64. Preparation of 18 2-bromo-1,3-diphenylpropane (Formula D-2; where R is dibenzylmethyl) See D Drawing_ To a flame-dried flask equipped with a reflux condenser * 2.12 g of 1,3-diphenyl-propan-2-enzyme for the preparation of 17 was added under an argon atmosphere. Fermented with 0.32 ml of tribromo ... ............ Refer to ............... ......... tr ........... Factory Green (Please read the &amp; notes on the back before filling in this page) -105- This paper uses China as the standard Standard (CNS) A4 Specification (210X297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A6 ___B6__ V. Description of the Invention (104) Phosphate M is slowly treated in a dropwise manner. Once the addition is completed, this exothermic mixture will change It becomes cloudy and becomes a two-phase system. After 1 hour, the reaction is partitioned between diethyl chain-hexane and water. The organic phase is diluted with sodium bicarbonate aqueous solution, washed with ascites, dried (magnesium sulfate), and sprayed under reduced pressure *懕 The cold titled product produced 2.08 g of crude title product * as a viscous brown oil. The crude auspicious compound can be used directly in the next preparation without further passivation. Example 16 4-Hydroxy-3- (1,3-diphenyl) Propyl) -coumarin (Formula D-3; where R is 1,3-diphenylpropyl) See D. For a flask containing 485 g of 4-hydroxycoumarin of formula D-1 * Add A total of 2.08 g of crude 2-bromo-1,3-diphenylpropanamidine from Preparation 18 was produced. Add the resulting condensate to a chilled condensate tube and heat to 130t: —Night. The reaction mixture is cooled to room temperature * and partitioned between diethyl g and 1M sodium hydroxide; washed with diethyl K diethyl® and K6N hydrochloric acid After acidification to = 1, M digas methane (formaldehyde-chloroform as latent solvent) was repeatedly extracted. The dichloromethane extract of the mixture was diluted with aqueous sodium bicarbonate solution, washed with brine, and dried (magnesium sulfate). Concentrated under reduced pressure. The residue was adsorbed on silica, and then subjected to rapid column decantation with 40% to 60% ethyl acetate / hexane to produce 32 mg of 檷 S product as a ocher solid. /.: Physical properties As follows: XH NMR 8 7.72, 7.49, 7.39-7.14, 6.73, 4.65, 2.86-2.66, 2.51; EI-MS M + = 356.1410 (real jump value>). Preparation of 19 2-cyclohexyl-1-phenylethanol p-flame In a dry flask, add 5.4 grams of pyridinium chlorochromate and 20 liters of two atmospheres (please read the precautions on the back before filling in the first page. Packing ¥ -106- This paper size applies to national standards (CNS) A4 specification (210X297mm) A6 B6 5. Description of the invention (105) Methane. The resulting orange suspension M0.7 ml of commercial 2-hexylacetone After 3 hours, the brown mixture was filtered through a Cypriot dish, using dichloromethane as a lotion. The filtrate was washed with dilute hydrochloric acid, dilute aqueous sodium bicarbonate solution, deionized water, and dried (magnesium sulphate). Dish filtered. The light brown solution was cooled to 0 * C under argon atmosphere, and then 5.0 ml (3.0 M in diethyl ether, phenylmagnesium bromide was slowly treated. The reaction mixture was allowed to warm to room temperature. The material was then diluted. Ammonium hydroxide aqueous solution, saturated ammonium vaporization, brine washing, drying (magnesium tellurate) and concentrated under reduced pressure. The residue is analyzed by 15% to 25% diethyl ether / hexane in a fast column, which can produce 1.01 The title product is a viscous, clear pleated oil. Physical properties are as follows: 1 NMR 5 7.40-7.21, 4.28, 1.81-0.86. Example 17 3- (2-cyclohexyl-1-phenylethyl) -4- Hydroxycoumarin A dry-filled flask containing a mixture of 650 mg of 4-hydroxymyristole and 1.01 g of 2-cyclohexyl-1-benzyl ether (Preparation 19) in 20 ml of dioxane, added under argon atmosphere 2.5 ml of trifluoride touch etherate. The resulting yellow solution was allowed to stir at room temperature overnight. The volatiles were removed and the residue was partitioned between diethyl ether and 1% sodium hydroxide. The alkaline aqueous phase was diethyl ether. Washed with 6N salt, printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs {Please read the precautions on the back before filling this page)-Pack Acidified to a = 1. The resulting precipitate was repeatedly extracted with dichloromethane (formazan-gasoline as a latent solvent). The mixed dichloromethane extract was diluted with sodium bicarbonate to remove most of the unreacted 4-hydroxycoumarin, and then washed with brine, dried (magnesium sulfate), and finally concentrated under reduced pressure. . The residue was adsorbed on silica and K 3 0% to 60% ethyl acetate / hexane was subjected to flash column chromatography 'to produce 110 mg of the title substance as a brown solid. -107- The paper size aii + as household materials (Gusm County · Moxm Co .; ^ V. Description of the invention (106) A6 B6 The physical characteristics are as follows: XH HMR δ 7.71. 7.53-7.20, 6.67, 4.75, 2.13-0.93; economic Ministry of Central Standards Bureau, Behr Consumer Cooperative, Inle IR (Reconciliation) 3217, 2924, 1673, 1623. 757 cm-1; EI-HS M + = 348.1724 (real value). Preparation 20 1- (4-methylbenzyl Base) Ding-bufer dry flame beaker * Add 0.59 ml of commercial p-tolualdehyde and 15 ml of tetrahydrofuran under argon atmosphere. The solution is cooled to ου * and M3.0 ml (2.0 M / diethyl ether) Treatment with propylmagnesium bromide. The reaction mixture was allowed to warm to room temperature overnight. It was stopped by adding ammonium chloride aqueous solution. After diluting with κdiethyl ether, the phases were separated. There was 榇 phase Κ saturated ammonium chloride, 迩 washing with water, It was dried (magnesium sulphate) and concentrated under reduced pressure. The residue was analyzed by flash column using 20% to 30% diethyl ether / hexane to produce 980 mg of the title compound as a clear, colorless oil. Physics The characteristics are as follows: 1 NMR S 7.22. 4.62, 2.33, 1.86-1.26, 0.92. Example 18 4-Hydroxy-3- (1- (4-methylphenyl) -butyl) -coumarin In a flame-dried bottle containing 650 mg of 4-hydroxycoumarin and 980 g of Ketobu (4-methylphenyl) -butan-1-enzyme (Preparation 20) in a mixture of 20 ml of dioxane, Add 2.5 奄 liters of trifluoride trifluoride in the atmosphere of M. The resulting yellow solution was allowed to stir overnight at room temperature. The volatiles were removed • and the residue was partitioned between diethyl ether and 1 珩 tritium hydroxide, sickle It was washed with diethyl ether and acidified with M6N hydrochloric acid to = 1. The resulting precipitate, M dichloromethane (Shenzhen-chloroform latent solvent), was quickly extracted. The mixed dichloromethane extract, Kleen-108-, please (Please read the notes on the back before filling this page) Binding &quot; This paper size is not applicable. China National Standard (CNS) A4 Specification (210X297mm) 'A6 B6 Printed by the Offshore Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Description of the invention (107) The sodium bicarbonate was washed once to remove most of the unreversed 4-transcoumarin, washed with K brine, dried (magnesium sulfate) and finally concentrated under depressurization. The residue was adsorbed To silica, and flash column chromatography with 40% to 50% ethyl acetate / hexane, K yielded 660 g of gadolinium product, White gambling. Physical properties are as follows: aH NMR 6 7.84, 7.8, 7.47, 7,39, 7.22, 7.13. 4.60, 2.30, 2.15, 1.42, 0.96; IR (reconciled) 2955, 2925 · 2857, 1666, 1607 cm- 1; EI-MS M + = 308. 1400 (found). Preparation 21 1- (4-Ethylphenyl) -but-1--1-enzyme In a flame-dried flask, 0.69 ml of commercial 4-ethylbenzaldehyde and 15 ml of diethyl ether were added under an argon atmosphere. The solution was cooled to 01C * and treated with M30 奄 L (2.0 M / diethyl ether) propylmagnesium bromide. The reaction mixture was warmed to room temperature overnight, and then stopped by adding an aqueous ammonium solution. After dilution with M diethyl ether, the organic layer was washed with saturated ammonium dichloride, dried (magnesium sulfate), and finally concentrated under reduced pressure. The residue was subjected to flash column chromatography using 25% to 30% diethyl ether / hexane to give 1.08 g of the title product as a clear, colorless oil. The physical properties are as follows: ~ 1 NMR δ 7.28-7.15, 4.62 and 4.60, 2.63. 1.90, 1.79-1.61, 1.5-1.2, 1.22, 0.90. Example 19 3- (1- (4-Ethylbenzyl) -butyl) -4-hydroxychromanin pair contains 325 mg of 4-hydroxycoumarin and 500 mg of (4-ethylphenylbutane- 1-alcohol (Preparation 21) was added to a flame-dried flask with a mixture of 10 ml of dioxane. 1.25 ml of boron trifluoride etherate was added under an argon atmosphere. Generated: -109- This paper uses Chinese national standards (CNS) A4 specifications (210x297 mm) {谙 Read the precautions on the back before filling the nest sheet) .0. .Booking and Ordering Ministry of Economics &quot; Stamp of the Consumer Standards Cooperative of the Central Bureau of Standards * Α6 Β6 V. Description of the Invention (108) The yellow solution was allowed to stir at room temperature for two nights. Volatile matter was removed * The residue was partitioned between diethyl ether and 1N sodium hydroxide. The sickle aqueous phase was washed with diethyl ether and then acidified with K 6N hydrochloric acid to give = 1. The resulting precipitate, K 2 gas methane (formazan-ambient latent solvent) was repeatedly extracted. The mixed two-gas methane extract was washed once with dilute hydrogen carbonate to remove most of the unreacted 4-hydroxycoumarin ', washed with brine, dried (magnesium sulphate), and finally poured under reduced pressure. The residue was subjected to flash column chromatography with 40% ethyl acetate / hexane * to produce 360 mg of the title product * as a white imagination. The physical properties are as follows: NMR δ 7.85, 7.49-7.33, 7.26-7.20, 7.12, 4.49 and 4.46, 2.59, 2.36-2.26, 2.19-2.08, 1.42- 1.36, 1.20, 0.96; IR (harmonic) 2956, 2927, 2871, 1663, 1605, 1454, 1378 cm &lt; EI-MS M + = 32. 1561 (measured value). Preparation 22 1- (1-naphthyl) -propan-1-enzyme in a flame-dried dry flask containing 8.0 ml of anhydrous tetrahydrofuran, cooled to -78 t under argon atmosphere, and added 4.0 'ml (3.0 M) Ethylmagnesium bromide / tetrahydrofuran solution. Stirable solution K 136 g of a commercially available solution of 1-naphthaldehyde / 4.0 ml of tetrahydrofuran. The reaction was stirred at -781C for 5 minutes and then warmed to room temperature. After 1 hour the mixture was cooled to 0 ° C. Be careful to stop with saturated ammonium and dilute with diethyl ether. Separately, wash organically with hydrophilic, dry (magnesium sulfate) and concentrate under reduced pressure. The residue was subjected to flash column chromatography using 25% ethyl acetate / hexane to produce 1.76 g of the title product light pink -110- This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) (please (Please read the notes on the back before filling this page). Binding. Ordering A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (109) Oily. The physical properties are as follows: ^ NMR δ 8.08, 7.85, 7.75, 7.60, 7.52-7.23, 5.36 and 5.34, 2.14, 2.02-1.62, 0.94 ° Example 20 4-hydroxy-3- (1- (naphthyl) -propyl) _ Coumarin to 324 mg of 4-hydroxycoumarin and 3 7T g of 1- (1- (bonaphthyl) _propan-1-ase (Preparation 22) in a turbid solution of 7 ml of dioxane under argon atmosphere Add 0.85 liters of trifluorinated etherate. After soaking overnight, the resulting yellow solution was concentrated under reduced scraping. The residue was partitioned into water and ethyl acetate; washed with organic M salt and dried (magnesium sulfate) And concentrated. After the residue was adsorbed to silica gel, 40% to 50% ethyl acetate / hexane was used for flash column analysis to produce 337 mg of the title product as a pale yellow solid. Crystallized to make analytical grade samples. Physical properties are as follows: (Μ. P. 200-202¾): ^ XH NMR δ 8.10, 7.88-7.81, 7.59-7.41, 7.27, 7.13, 6.74, 5.13, 2.42-2.21, 1.18; IR (Reconciliation) 3234 ,. 2954, '28 to 5, 1,678, 1622, 1610 cm-1; FAB-MS [m + H] = 331 (measured value) ° Example 21 3- (1,2-diphenyl Vinyl) -4-hydroxycoumarin To a flame-dried flask containing 650 mg of 4-hydroxymyristotin and 1.0 g of a commercially available trans-monooxide in a 20 ml dioxane mixture, add 2.5 liters of boron trifluoride etherate (under an argon atmosphere). 。The yellow solution produced makes it available in the room._11 The paper size of the paper uses the national standard (CNS) r4 specification (210X297 mm) '[谙 Read the precautions on the back before filling in this page} 0 — .Binding economy Printed by the Ministry of Health, the Central Bureau of Quasi-Bureau Consumer Cooperative, A6, B6 5. Description of the invention (110) Sowing overnight at warm temperature. The volatiles are removed, and the residue is distributed in diethyl ether and 1N sodium hydroxide. The hydrographic test K Washed with diethyl ether and acidified with K6N hydrochloric acid to yield = 1. The resulting precipitate, M dichloromethane (methanol-aqueous latent solution_ &gt; repeated extraction. The mixed dichloromethane extract, M, dilute hydrogen carbonate— Most of the unreacted 4-hydroxycoumarins were removed in the second time, and then dried (magnesium sulfate), and finally concentrated under reduced pressure. The residue was 50% to 66% ethyl acetate. / Hexane line flash column analysis, can produce 880 mg of the title product as a white solid. The physical properties are as follows: HMR δ 7.48, 7.14, 7.06-6.82, 6.31; 13C NHR δ 16Γ, 160, 152, 147, 142, 140, 131, 129, 128 (2), 127, 123 (2), 117, 116 (2), 103; IR ( Reconciliation) 2954. 2925, 2855 · 1670, 1611, 755, 701 cm-1; EI-MS H + = 340 (measured value). Preparation 23 3- (3-cyano-phenyl) -but-2-enoic acid tert-butylphosphonium ester (Formula E-2

) Refer to Figure E. For the flame 'dry three display and bottom bottom flask equipped with a reflux condenser, add 880 mg (60% dispersed phase in mineral oil) of sodium hydride and 10 ml of anhydrous benzene under argon atmosphere. The rhenium suspension was cooled to Ot; and M4.2 liters of tertiary butoxycarbonyl-methylphosphonic acid dimethyl was treated dropwise. The rate of addition can control the evolution and exotherm of the gas. After 10 minutes, the mash was warmed to room temperature. After 1 hour, the solution was cooled to 0 ° C. and treated with 2.90 g of a commercially available formula of E-1 3-ethenylbenzonitrile (though solid). The wall of the reaction flask was wetted with 5 ml of water. Once -112- This paper size applies to China National Chess Standard (CNS) A4 specifications (210X297 male: '' (谙 Please read the precautions on the back before filling in this page). Installed. -SJ. A6 B6 Ministry of Economy Printed by Standard Bureau Shellfish Consumer Cooperative Co., Ltd. 5. Description of the invention (ui) The reaction was warmed to room temperature, and the mixture became cloudy due to the formation of precipitates. After standing at room temperature for 1 hour, the reaction was heated in an oil bath at 80 ° C for one night. The gelatinous residue was cooled to room temperature, and then partitioned into diethyl ether and dilute potassium hydrogen sulfate aqueous solution. The aqueous layer was extracted with two additional portions of diethyl ether. The mixed diethyl ether extract was dried over magnesium sulfate. The radon residue was concentrated and purified on silica gel under reduced pressure and purified by flash column chromatography. K10% to 15% ethyl acetate / hexane was used to dissolve the diastereomeric product of 4.30 g of the titled product as a light brown oil. Isomer 3: 1 Primary: minor isomer ratio &gt; Physical properties are as follows: _ 'H NMR (CDC13) 5 7.74-7.43, 6.06, 5.90, 2.53, 2.13, 1.52, 1.27 ° Preparation 24 3- ( 3-cyano-phenyl) -butyric acid tert-butyl hydrazone (formula E-3) see figure E. For an e-bottle containing 500 mg 5% Pd / C, add 4.30 g of 3- (3-cyanophenylbut-2-enoic acid third butyl ester (Preparation 23) was added as a solution in 15 ml of ethyl acetate. The reaction mixture was shaken overnight at 45 Psi hydrogen The resulting black slurry was filtered through a plug, and the filter cake was washed with ethyl acetate. The combined filtrate was shrunk under reduced pressure to produce 4.30 g of the title product as a clear, colorless oil. The physical properties are as follows: ^ HMR ( CDC13) 5 7.54-7.37, 3.28, 2.51, 1.34. 1.30 ° __ Preparation 25 3- (2-carboxy-1-methyl-ethyl) _benzoic acid (Formula 4) See Table 1. For 1.09 g of 3- ( 3-cyano-phenyl) -butyric acid tert-butyl _ (Preparation 24) in (Please read the notes on the back before filling in this page) e: • Binding. _113_ This paper size applies to China's family standard ( CNS) A4 specification (210X 297 mm) 5. Description of the invention (112) A6 B6 1.0 liters of stirred solution of acetic acid, add 5.0 ml of 30% osmium potassium oxide aqueous solution. The resulting mixture is heated at 701: 3 days The reaction was cooled to room temperature and washed twice with K diethyl ether. The aqueous layer was acidified with aqueous M1H hydrofluoric acid to give out = 2. The resulting precipitate K was extracted with chloroform containing formazan * until no substance was desired The thin-walled decantation is known as the chloroform extract of the port at the end of the water calendar. It was dried on magnesium sulfate, and was finally concentrated under reduced pressure to produce 0.67 g of the title product as a light ocher solid. The physical properties are as follows : ^ NMR (CDC1a-CDaOD) 5 7.92, 7.46. 7.38, 4.88, 3.34, 2.62, 1.34; {谙 Please read the notes on the back before filling in this page} EI- printed by Shellfish Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs MS: [M *] = 208.0755 (real value). Elemental analysis, found C, 63.42; H, 5.78. Preparation 26 3- (2-Third-butoxycarbonyl-methylmethyl) -benzoic acid tert-butyl ester (formula E-5) See Figure E for a pair containing 2.71 g of 3- (2-carboxy-1-methyl- Ethyl) -benzoic acid (Preparation 25) in a 40 ml digas methane suspension flask, charged with isobutylene gas through a Clayson head adapter. The gas was condensed into liquid on the dry ice-acetone cold finger valve and dropped into the reaction vessel until the reaction volume was approximately doubled. The addition of isobutene was stopped * and the resulting brown solution was allowed to sow at room temperature overnight. The reaction mixture was slowly added to an excess of saturated sodium bicarbonate and partitioned into diethyl ether. The aqueous layer was re-extracted in three portions of diethyl ether. The combined diethyl ether layer was washed with water, dried over magnesium sulfate, filtered off and finally concentrated under reduced pressure. The resulting residue M was purified by 5% to 10% ethyl acetate / hexane on a silica gel flash column chromatography to produce 2.38 g of the title product. In order to clarify the light color -114- This paper standard uses the National Standard (CNS) A4 specifications (210X297). A6 B6 Employee Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. Printing 5. Description of the invention (113) Oil 〇 .. The physical properties are as follows: 'H HMR (CDC13) S 7.83, 7.36, 3.28, 2.51, 1.60, 1.35, 1.28; EI-MS: [Μ · -15] = 305 (measured value). Preparation 27 3-[ 2-Third-butoxycarbonyl-3- (2-hydroxy-phenyl) -p-methyl- 3-oxy-propyl] -benzylcarboxylic acid tert-butyl hydrazone (formula E-6) see 阄 E under argon In the flame-dried flask, 1.40 ml of diisopropylamine and 10 liters of anhydrous tetrahydrofuran were added. The solution was cooled to -78t: and treated with K6.20 liters (1.6 M in hexane) of n-butyl lithium. The solution was warmed After 30 minutes, it was cooled to -78 TC. Lithium diisopropylamine was dissolved to obtain M. 98 g of 3- (2-tert-butoxycarbonyl-bumethyl-ethyl) stearic acid tert-butyl ester ( Preparation 26) treatment, the latter was immersed in 6.0 ml of anhydrous tetrahydrofuran (1.0 liters of wet) solution and carried through a catheter. The resulting fresh yellow enoate solution was stirred for 45 minutes, and then K 0.40 ml of methyl salicylate Processing, the latter presented at 2.0 A solution of ml of tetrahydrofuran (1.0 ml of wet) was passed through the catheter. The resulting reddish reaction mixture was allowed to warm its temperate to room temperature overnight. The reaction mixture was then condensed under reduced pressure and partitioned with ethyl acetate and cold. In dilute aqueous hydrochloric acid solution. Extraction was performed in two portions with ethyl acetate. The combined ethyl acetate extract was washed with brine, dried over magnesium sulfate, filtered, and finally concentrated. The resulting residue, Ml, was 10% to 25% ethyl acetate / hexane was passivated on a silica gel for flash column chromatography and passivated to yield 0.895 g of the diastereoisomer of the title product as a light oil (S 3: 1 major: minor isomer type Proportion). The physical characteristics are as follows: f Please read the notes on the reverse side before filling in this page} Φ .. -Binding-115 · This paper size applies to China National Standard (CNS) A4 (210X297mm) A6 B6 Printed by the Consumer Cooperative of the Central Bureau of the Ministry of Economic Affairs V. Invention Description (114) XH HMR (CDCI3) 5 12.19, 11.88, 8.0-6.9, 4.62, 4.56, 3.86, 1.61, 1.56, 1.43, 1.40, 1.27. 1.07 Preparation of 28 3- [1- (4-hydroxy-2-oxy-2H-chromen-3-yl) -ethyl] benzene Acid (formula E-7) reference gas · E-pair containing 187 mg to prepare 27 ^ 3- [2-third butoxy truncyl-3- (2-phenyl) -1-methyl-3-oxy -Propyl] -benzoic acid tert-butyl ester flask, 2.0 liters of trifluoroacetic acid was added. The resulting brown solution was allowed to stir at room temperature. After 14 hours, the reaction turned milky with a large white precipitate. The reaction mixture was concentrated under reduced pressure and triturated with toluene (3x) to remove the residual trisoxygenic acid, yielding 124 mg of the title product as an off-white solid. The physical properties are as follows: ^ HHR (d7-DMF) S 8.05, 7.85, 7.64, 7.30, 4.75, 1.76; EI-MS: [M *: I = 310.0841 (measured value). Example 22 4-Hydroxy-3-U- [3-[[[((l, dimethyldimethylethoxycarbonyl) methyl] limyl] carbonyl] phenyl] ethyl] -coumarin] prepared 46 mg 28 Product of the question, 30 g of tertiary butyl glycine hydrochloride and 60 microliters of diisopropylethylamine ', mix with 0.5 milliliters of dichloromethane ... Add to the solution, add 30 liters of diethyl cyanophosphonate. The mixture was allowed to sow at room temperature overnight. Reaction M was diluted with dichloromethane, and washed with aqueous HCl solution, water and finally brine. Dichloromethane belongs to magnesium sulfate. Filter and finally shrink under reduced pressure. The residue was purified by flash column chromatography on silica from 5% to 8% methanol / dichloromethane to yield 48 mg of the title product as a white solid. (I first read "Notes on the back side and then fill out this page). Binding-Binding--116- Not applicable to China Forklift Paintings" Jia Chouge (210 — Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs System A6 B6 V. Description of the invention (115) The physical properties are as follows: HHR (CDCl3) 5 7.83, 7.46, 7.20, 4.60, 4.13, 1.64, 1.47; FAB-MS: [Μ + Η] = 424 · 1733 (measured value) Preparation of 29 (E and Z) -3- (3-nitrophenyl) -pent-2-enoic acid tert-butylphosphonium (Formula F-2 &gt; see figure F under argon) • Sodium hydride (1.0 g of 60% oil-dispersed phase) floated in 25 ml of benzene, and placed in a dry three-necked tritium flask equipped with a liquid addition funnel, an argon inlet, and a temperature probe for radon. The flask was immersed in an ice bath and magnetically broadcast there. In the suspension: • Add 4.8 liters of P, P-dimethylphosphonic acid. The third butyl ester acid (pure) through the addition funnel. The rate of addition is adjusted to the reaction temperature can be maintained at 10-151C After the addition is complete, remove the ice bath and stir the mixture at room temperature for 60 minutes. Afterwards • Quickly add 4.48 grams of commercially available finely divided formula F-1 via the reaction vessel's neck *. -Nitroethyl Base powder. The reaction mixture turned dark immediately and dissipated heat, and magnetic stirring could not be done immediately. The dark gel immediately formed and the M spatula was broken (so as to minimize exposure to the atmosphere), and the reaction was stirred as much as possible overnight. The next day, the mixture was separated into ethyl chain and aqueous sodium hydrogen sulfate solution. The organic phase was washed with brine and dried (magnesium sulfate). The solvent was removed under reduced pressure, and the residue was 10% ethyl acetate / hexane. Silicone 60 (230-400 mesh) rapid decantation in the upward direction can produce 6.16 grams of rubbing product as a yellow oil. E / Z isomers can be separated by KI, but this is not necessary because the two are in the next chemistry The steps are converted into the same product. The physical properties of the A isomer are as follows: -117- This paper size uses China. National Standard (CNS) A4 specification (210X297 mm) (谙 Please read the precautions on the back before filling Nest page}. Binding: printed by A6 _ B6___ of the Consumers 'Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (116)' H HMR δ 1.08, 1.53, 3.10, 6.00, 7.57, 7.76, 8.21, 8.29 〇IU0 .38 (15% ethyl acetate / hexane) The physical properties of B isomer are as follows . AH NHR δ 1.07, 1.24, 2.46, 5.89, 7,5, 8.03, δ 17 square 0.32 (15% ethyl acetate / hexanes> spirits to give E / Z mixture of the title product from the reaction of the following physical properties:

El MS 277 〇 IR 2977, 1712, 1531, 1349, 1150 cm-1. Analytical measured values: C, 64.95; H, 6.93; 5.04. Preparation 30 3- (3-Aminophenyl) valeric acid third butyl ester (Formula F-3) See Figure F. For 4.64 g of 29 starting bondene, in 40 ml of formic acid solution, add 260 奄G 5% Pd / C. The mixture was placed in a Yere unit and shaken overnight at 50 psi hydrogen. The next day, GC analysis showed that Gu was incomplete. Add platinum oxide (200 mg). Shock «consumption under 50 psi hydrogen. After a few hours * GC showed complete response. The mixture was filtered through a plug, acetic acid • a ethyl acetate was moistened, and the filtrate was shrunk under reduced pressure to produce 4.15 g of the title product as a brown oil. The physical properties are as follows: 1H NMR δ 0.79, 1.34, .1.6, 2.5, 2.85, 3.6, 6.5, 7. 1 〇

El MS 249 ° -118--This paper size is applicable to China National Standard (CNS) A4 specification (210X 297 mm). (谙 Read the notice on the back and fill in this page first) 0. • Binding. Ministry of Economic Affairs Printed by A6 _B6_ of Consumer Cooperatives of the Central Bureau of Standards 5. Description of the invention (117) Preparation of 31 3- (3-triphenylmethylaminophenyl) valeric acid third butyl ester (formula F-4) 4.15 g of a starting solution of 30 starting amines and 3.5 ml of diisopropylethylamine / 40 ml of dichloromethane were added to 5. 10 g of chlorotribenzyl chloride and added in portions within about 10 minutes. Note that To slightly exothermic. The resulting solution was stirred at room temperature overnight. The next day, the solvent should be removed and the residue was partitioned between ethyl acetate and cold water. The aqueous layer was extracted with another portion of ethyl acetate and mixed. The organic layer was washed with brine and dried (magnesium sulfate). After the solvent was removed under reduced pressure, the residue was quickly analyzed on silica gel with M10% ethyl acetate / hexane. This gave 8.75 g of the title product as a white color. The physical properties are as follows: 4 NHR S 0,57, 1.3, 1.36, 2.24, 2.55, 5.01, 6.14, 6.25, 6.40, 6.86, 7.2-7.4.

El MS 491. IR 3418, 2958, 2925, 2856, 1729, 1602, 1485, 1446, 1153, 1145, 702, 698 cm-1. TLC Rr 0.32 (10% ethyl acetate / hexane) Anal. Found: C, 83.01;, 7.70; H, 2.87. Preparation 32 3- (3-triphenylmethylaminophenyl) -2- (2-hydroxybenzyl) valeric acid third butyl ester (Formula F-5) See F under argon, 250 To a dry flask of a milliliter round bottom flask, 25 milliliters of anhydrous tetrahydrofuran and 3.7 milliliters of anhydrous diisopropylamine were added. The solution was cooled to -78 t * and a 1.6 M butyllithium / hexane solution was added via a syringe M for several minutes. The solution is warmed to 01, and kept at this temperature for several minutes, and then cooled to -78 -119- ^ This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) Refill the book and buy one. Pack. Order. Printed by the Central Standards Bureau of the Ministry of Economic Affairs, Behr Consumer Cooperative A6 _B6__ V. Description of the invention (118) In this soaking solution of lithiated diisopropylamidine, introduce 8.2 Grams of a solution of 31-trityl third butyl ester in 25 liters of anhydrous tetrahydrofuran, and K1 of 4 ml of solution to wet the raw material bottle. Let 50 minutes of ene fermentation at -78¾, can produce Red orange solution, 1.1 ml of methyl salicylate was added dropwise via a syringe. After 5 minutes sickle, the cold solution was warmed to the ring temperature. The reaction color changed to _dark red * and then S texture faded overnight. The next day * The reaction mixture was partitioned into ethyl acetate and ice water containing 100 liters of 7 phosphate buffer solution and 50 liters of 1 M potassium hydrogen sulfate aqueous solution. The value of the aqueous layer was nearly neutral at this point, and ethyl acetate was once again Ester extraction removes all active substances. Dry mixed organic mash (magnesium sulfate) TLC (10% ethyl acetate / hexane) at this point showed two stickiness: A (more mobile, 0.36, equivalent to the expected starting material for preparation 31), and B (less mobile) , Rf 0.24, equivalent to the title product) 〇 Remove the solvent under reduced pressure to produce the desired product and a crude mixture of orange red foam at the beginning. This mixture is on a silicone 60 (230-400 mesh sieve) K 60- A 70% dichloromethane / hexane line was quickly analyzed to produce a clean product separated from the starting material. 944 mg of the desired title product was obtained in the form of a dark brown broken foam, and 86 9 mg of the starting material of Preparation 31 were obtained. The starting material can be recycled. The physical properties of the product (mixture of diastereomers) are as follows: HMR δ 0.41, 1.13, 3.19, 4.28, 6.25, 4.48, 6.8-7.0, 7.2-7.4, 7.5 · 7.84 ° -120- This paper size applies to China National Standard (CNS) A4 specification (210X297mm) {Please read the precautions on the back before filling out this page}-Binding. A6 B6 V. Description of Invention (119) PAB MS [丨 + H] = 612. Anal. Found: C, 78.91; H, 6.72; U, 2.21. Preparation 33 3- [1- (3-Aminobenzyl) propyl] -4- Hydroxymyristotin (Formula F_6) is shown in Figure F. To 918 mg of Preparation 32 of the title product, 6 ml of trifluoroacetic acid (TFA) was added. A bright yellow-orange color was formed immediately, and the solid was dissolved. The solution was stirred at room temperature for 24 hours. Hours. TFA was removed under minus®, and the residue was partitioned between dioxane and cold 7-phosphate slow street solution, and a sufficient amount of sodium hydroxide aqueous solution was added to make the water calendar neutral. The two-phase hydrazone mixture containing a small amount of undissolved solids was placed in a continuous ore extractor and extracted with a foamed di-aerated methane stream overnight. When the aqueous layer no longer shows the hydration tertiary activity, the fermented extract is removed and dried (sodium sulfate). The solvent was removed under reduced pressure, and flash column chromatography was performed on a silica gel 60 (230-400 mesh sieve). Prepare by flash column and dissolve first 30% ethyl acetate / dichloromethane. Then it is dissolved with 50-100% ethyl acetate and pure 5% formic acid / ethyl acetate. The product fractions were combined and concentrated to give 369 mg of the title product as a brown solid. 'The physical properties are as follows: HMR δ 1.02, 2.12, 4.41, 4.6, 6.60, 6.75, 6.88, 7. 1-7.3, 7.48, 7.71. El MS: 295. 1213, 266. TLC Rf 0.24 (30% ethyl acetate / dichloromethane). Printed by the Shellfish Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before writing this page). Installation Example 23 4-hydroxy-3- [1- [3-[[3-[(1,1 -Dimethylethoxycarbonyl) amino] -1-ketopropyl] amino] phenyl] propyl] -myristotin 制备 22.2 mg to prepare 33 amines and 18.5 mg Boc- / S-alanine in- 121- This paper size is applicable to National Standard (CNS) A4 specifications (210X297 mm) A6 B6 V. Description of the invention (120) 0.5 ml of cold (Ot :) soaking solution of diazomethane, add 17 micron Liters of diisopropylethylamine. Add 14 microliters of diethyl cyanophosphate. The solution was stirred * and allowed to warm slowly overnight. The reaction mixture was subjected to flash chromatography on silica gel with 80% ethyl acetate / dichloromethane * and 2-4-8-1 2% formic acid in this solvent to produce 26.6 mg of the title product * as glass.状 Solid. The physical properties are as follows: HHR 6 0.79, 1.28, 2.0-2.5, 3.25, 4.30. 6.8- 7.3, 7.8 ° Example 24 3- [1- [3-[(3-Amino-butanylpropyl) amino] Phenyl] propyl] -4-hydroxy-coumarin trifluorophosphonium trifluoride, 10.2 g of the solution of the product of Example 2 3 in 0.5 ml of trifluorophosphonic acid * Let it stand at room temperature for 20 minutes, then Μ Dichloromethane was diluted and concentrated under reduced pressure. The residue was dissolved in 0.5 l of water, and the solution was freeze-dried to produce 11.1 mg of the title product as a flocculent white solid. The physical properties are as follows: FAB HRMS [m + H] = 367.1644. Example 25 4-Hydroxy-3- [l- [3-[(1-oxy-3-benzylpropyl) amino] benzyl] propyl] -carnodin 'Consumption by Shellfish, Central Bureau of Standards, Ministry of Economic Affairs Printed by the cooperative {谙 Please read the precautions on the back before filling in this page}. Pack ¥ To 22.2 mg of the preparation of 33 amine and 15 g of hydrocinnamic acid in 0.5 ml of an ice-cold (0Ό) stirred solution of dinitromethane 17 microliters of diisopropylethylamine and 14 microliters of diethylcyanophosphate. The solution was stirred and warmed slowly overnight. The reverse reaction mixture was subjected to flash chromatography on a silica gel. M 20% ethyl acetate / dichloromethane and subsequent 2-5% methanol were dissolved in this solvent to produce 23.3 mg of the title product. • A glassy rose solid. -122- This paper size is in accordance with China National Standards (CNS) Henry 4 Specification (210X297 Gong 1 No. 83100644 Patent Application Inspection Chinese Manual Correction Page (August 1985) A7 B7 Employee Cooperation Cooperation of the Central Standards Bureau of the Ministry of Economic Affairs The fifth, description of the invention uvl) The physical characteristics are as follows: XH HMR 3 0.95, 2.1-2.4, 2.6, 3.0, 4.32, 7.1- 7.3, 7.45, 7.55, 7.84 ° El MS 427 〇 Example 26 -66 Use Similar to the above steps, other compounds of the present invention under K can be prepared, and their mass spectral data are shown in Table I below. 26) Coumarin, 3-[[[[[[((_ 2--benzimidazolyl) methyl] amino] carbonyl] phenyl] ethyl] -4-hydroxy- 27) Coumarin * 4-hydroxy-3- [1- [3-[[[(2-pyridyl) methyl] amino] carbonyl] phenyl] ethyl] -28) coumarin, 4-hydroxy-3- [b [3-[[(phenylmethyl) amino] carbonyl] benzyl] ethyl]-29) benzamidine, amidine-(2,3-dihydro-2 -hydroxy-1 fluorene -indene-: 1 -Yl) -3. [1- (4-hydroxy-2-oxy-2H-1-benzopiperan-3-yl) ethyl] -30) benzamidine, 3- [1- (4- Hydroxy-2-oxy-2Η-1-benzopiperan-3-yl) ethyl] -N- [2-methyl-1-[[(2-pyridylmethyl) .limyl] carbonyl] Butyl]-31) Coumarin, 3- [1- [3-[(Butylamino) carbonyl] benzyl] ethyl] &quot; 4-hydroxy- 32) Coumarin, 4-hydroxy-3- [1-[3-[[[((4-morpholinolyl) carbonyl] methyl] amino] carbonyl] phenyl] ethylphenyl 33) Coumarin, 3-U- [3-[[ [[[[(2-Benzoxazolyl) methyl] methyl] fluorenyl] carbonyl] methyl] limyl] carbonyl] phenyl] ethyl] -4-hydroxy- -123-Please read back Greed-Paper Paper Size Applies to Chinese National Standard (CNS) A4 Specifications 210X297 mm) No. 83100644 of the patent application, revised Chinese specification manual page (August 1985) A7 B7 V. Description of invention (d) Printed by the Central Government Bureau of Consumer Affairs, Ministry of Economic Affairs, Du printed 34) 4-hydroxy- 3- [ l- (l, 2,3,4-tetrahydro) -naphthyl] -coumarin 35) 4-hydroxy-3- [1-hydroimido] -coumarin 36) Coumarin, 3- ( a-ethyl-para-fluorobenzyl) -4-hydroxy-37) coumarin, 7-methoxy-3- (α-propylbenzyl) -4-hydroxy-38) 3-cyclopropane Phenylmethyl-4-hydroxy-7-methoxycoumarin 39) 3- (α, α-dimethylbenzyl) -4-hydroxycoumarin 40) Coumarin * 3- [1 -(3-aminophenyl) propyl] -4-hydroxy-, monohydrochloride "-. 41) Coumarin, 4-hydroxy-3- [1- [3-[[(1-naphthyloxy Methyl) carbonyl] amino] phenyl] propyl]-&lt; 42) aminocarboxylic acid, [1-[[[3- [1- (4-hydroxy-2-oxy-2fluorene-1-benzo] Piperan-3-yl) propyl] phenyl] amino] carbonyl] -2-methylpropyl]-, 1,: 1-dimethylethyl ester 43) Coumarin, 4-hydroxy-3 -[1- [3- [[[((1, Dimethylethoxycarbonyl) amino] methyl] carbonyl] amino] phenyl] propyl]-44) Coumarin * 4-hydroxy- 3- [1- [3- [(1-ketopentyl) amino ] Phenyl] propyl]-45) Coumarin, 4-hydroxy-3- [1- [3-[[((2-pyridyl) carbonyl] amino] benzyl] propyl] -46) Coumarin Flavin, 3- [1- [3-[[(aminomethyl) carbonyl] amino] phenyl] propyl] -4-hydroxy-, trifluoroacetate 47) Coumarin, 4-hydroxy-3- [lr {3- [n-oxy-3-methyl-3-[(1,1-dimethylethoxycarbonyl) amino] butyl] amino] benzyl] propyl]-48) Beans, 3- [1- [3- [(3-Amino-3-methyl-1-_butyl) -124-(Please read the note on the back # ^ before filling in this page) The paper size of the book is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83100644 patent application Chinese correction sheet (August 1985) A? —____. B7 V. Description of invention (\ Central Ministry of Economic Affairs Standard Bureau employee consumer cooperatives print amine] phenyl] propyl] -4-hydroxy-, trifluoroacetate 49) coumarin, 4-hydroxy-3- [1- [3- [U-oxy- 3-phenylpentyl) amino] phenyl] propyl-] 50) coumarin, 4-hydroxy-3-Π- [3- [[4- [(1, 1-dimethylethoxyfluorene) Group.) Amino] -1-ketobutyl] amino] phenyl] propyl]-51) Glutamine, N2-[(l,: l-dimethylethoxy) carbonyl]- K- [3- [l- (4-Hydroxy-2-oxy-2H-1-benzopiperan-3-yl) propyl] phenyl]-* 1,1-dimethylethyl ester 52) Glutamine , N- [3- [1- (4-hydroxy-2-oxy-2H-: l-benzopiperan-3-yl) propyl] phenyl]-, mono (-trifluoroacetic acid) salt 53 ) Coumarin * 4-hydroxy-3- [1- [3-[(1-oxy-4-phenylbutyl) amino] benzyl] propyl]-54) Coumarin, 4-hydroxy- 3- [1- [3- [U-oxy-5-phenylpentyl) amino] phenyl] propyl]-55) Coumarin, 4-hydroxy-3- [1- [3-[[ (Benzyl) carbonyl] amino] phenyl] propyl] -56) Coumarin, 3- [1- [3-[(3-cyclohexyl-1-ketopropyl) amino] phenyl] Propyl] -4-hydroxy-57) coumarin, 4-hydroxy-7-methoxy-3- [1- [3-[(1-oxy-3-phenylpropyl) amino] benzene [Propyl] -propyl] -58) coumarin, 4-hydroxy-3- [1- [3- [[3-[(1,1-dimethylethoxycarbonyl) amino] -oxopropyl] Amine] benzyl] propyl] -7-methoxy-59) propyridinecarboxylic acid, 2- [[[3- [1- (4-hydroxy-2-oxy-2Η-1-benzo) Piperan-3-yl) propyl] phenyl] amino] carbonyl]-, 1,1-dimethyl __- 125 -__ This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) ) &Quot; (Please Read the note at the back of the page ## Fill in this page again) Binding-Bookmark No. 83100644 Patent Application Revised Chinese Manual (August 85) A7 B7 V. Description of Invention (ι * // ·) Central Bureau of Standards, Ministry of Economic Affairs Employees' cooperative prints ethyl vinegar 6〇) amino formic acid, [2- [[3- [1- (4-hydroxy-2-oxy-2H-; L-benzopiperan-3-yl) propane Phenyl] phenyl] amino] -1-methyl-2-copperethyl]-, 1 f dimethyl ethyl ester 61) Propylamine, 2-amino-H- [3- [l- (4-Hydroxy-2-oxy-2H-benzophenan-3-yl) propyl] phenyl]-, mono (trifluoroacetic acid) salt 62) Coumarin, 4-hydroxy-3- 3- [ l- [3-[[3- (4-hydroxyphenyl) -1-_propyl] amino] phenyl] propyl]-^ ,. 63) Coumarin, 4-hydroxy-3-Π- [3- [[3- (1H-indole-1 -yl) -1-fluorenyl] amino] phenyl] propyl]-64) Myristotin, 4-hydroxy-3-Π- [3 -[[3- (1-naphthyl) -1-ketopropyl] amino] benzyl] propyl]-65) Coumarin * 3- [1- [3-[[3-[(2- Benzothiazolyl) fluorene] -1-S1propyl] amino] phenyl] propyl] -4-hydroxy-66) 4-hydroxy-3- [α-third-butoxycarbonylmethyl] benzyl Benzene preparation 34 1- (3-hydroxyphenyl) propanol (formula G-2) see figure G p-ethyl A solution of bromide magnesium (3.0 M in diethyl ether, 5.6 ml) in anhydrous tetrahydrofuran (5.6 ml) was added to a flame-dried flask under nitrogen and nitrogen at a temperature of 30 min. A solution of hydroxybenzaldehyde in anhydrous tetrahydrofuran (5 ml). The mixture was stirred for 30 minutes at op, and then carefully discontinued with a saturated aqueous solution of ammonium chloride (5 ml). The layers were separated, and the aqueous layer was extracted with diethyl ether (25 ml). The mixed organic layer was washed with κ brine (10 ml), dried over sodium sulfate, and concentrated under reduced pressure to form a light yellow semi-solid. (230-400 mesh sieve, 120 g) M ethyl acetate / hexane-126-(Please read the note on the back first ΫΓ · #: Then fill in this page). Packing. Standard (CMS) A4 specification (210 × 297 mm) A6 B6 Printed by the Consumers' Cooperative of the Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (125) (8 / 92-30 / 70) Gradient Rongxiong. Pooling JWTLC showed that (ethyl acetate / hexane, 25/75) had fractions with Rf = 0.18, and the solvent M was removed under reduced pressure to give the title compound. The physical properties are as follows: HMR (CDCU) 7.12, 6.77, 6.65, 4.43, 1.79-1.62. 0.87 δ ° Preparation of 35 1- (3-allyloxyphenyl) propionase (formula G-3) Preparation 34 1- (3-Hydroxyphenyl) propionase and anhydrous potassium carbonate (708 g) in a solution of anhydrous dimethylformamide (9.8 ml), in a flame-dried flask, and adding olefin under nitrogen Propyl bromide (0.44 ml). The resulting mixture was stirred at RT for 7 hours, diluted with EtOAc (65 ml), washed with water (30 ml) and brine (30 ml), and dried over anhydrous magnesium sulfate. 2. Concentrate under reduced pressure to form an oil, and then analyze it on a silica gel (230-400 mesh sieve, 100 g) M ethyl acetate / hexane (5 / 95-157 85) gradient lysate. Pool TLC (Z &lt; Ethyl acetate / hexane, 25/75) The fraction with Rf = 0.46 was measured, and the solvent was removed under reduced pressure to produce the title compound. The physical properties are as follows: CHH: Measured value ♦ · C, 74.δ 〇Γ H, 8.35. Example 67 3- (1,-(3-allyloxyphenyl &gt; propyl) -4-hydroxycoumarin (Formula G-4) See G diagram Contains 4-hydroxycoumarin U94 mg) and 1- (3-allyloxybenzene Base) Propanol (Preparation 35) was placed in a flame-dried flask of anhydrous dipyridine (17 ml), and the trifluoride etherate (1.92 ml) was added under nitrogen. The resulting solution was broadcast at RT. Mix for 24 hours, concentrate and remove the solvent. K dilute sodium hydroxide ~ (read the precautions on the back before filling the page). Packing -127- This paper size is applicable to National Standards (CNS) A4 specifications (210x297) A6 B6 printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs. 5. Description of the invention (126) (5%, 10 ml) diluted and extracted with 2 methane (2 x 50 ml). Mixed with 榇 蹰 M brine (20 liters) was washed, dried on sodium acetate, and concentrated to produce an oil, which was then chromatographed on silica gel <230-400 mesh sieve, 45 g), EtOAc / hexane The alkane (25/75) was dissolved. Confluence M TLC knows that fraction Rf = 0.22 (ethyl acetate / hexane · 50/50) 5 and removes the solvent to produce the title product. The physical properties are as follows: MS (EI) M * = 336.1371 »Example 68 3- (1- (3- ((2,3-dihydroxy) propoxy &gt; phenyl) propyl)-

4-hydroxycoumarin (Formula G-5) See G. 3- (1 '-(3-allyloxyphenyl) propyl) of Example 67 &gt; 4-hydroxycoumarin and 4-formaldehyde Chimorphine N-oxide (49 mg) in acetone / water (2.5 ml, 1: 1) mixture, androgen tetroxide (2.5 wU in tertiary butyrate * 35 μl) was added under nitrogen. The resulting The mixture was stirred at RT for 46 hours. At this time, 4-methylmorpholine If-oxide (35 grams) was added in one portion, and then condensed. K3H hydrochloric acid (1.5 ml) and sodium chloride were saturated. The solution was diluted with a saturated aqueous solution of sodium hydrogen sulfite, and extracted with ethyl acetate (4x10 liters). The mixed organic layer was dried over anhydrous 磙 _magnesium ... and concentrated under reduced pressure to form an oily film. «Preparative silica gel plate chromatography, M formase / chloroform (10/90) dissociation. Extract the band Rf = 0.17-0.29, remove the solvent under reduced pressure to form a thin film, which is again preparative silica gel plate at 20 00 α Chromatography 'Μ methanol / chloroform solvent (10/90 and 1_5 / 85). The title compound can be generated after extraction of fractions. The physical properties are as follows: -128- This paper scale applies Chinese National Standard (CNS) A4 regulation Grid (210X297 mm) [谙 Read the precautions on the back before filling out this page)-#. -Installation printed by A6 B6 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (12?) MS (El) = 370.1419 . Preparation of a solution of 36 1- (2-allyloxyphenyl) propionate p-2-hydroxyethylphenylphosphonium (2.00 g) and anhydrous potassium carbonate (5.52 g) in anhydrous dimethylformamide (20 ml) Under nitrogen, allyl bromide (1.38 ml) was added. The resulting mixture was stirred at JIT for 8 hours, concentrated to remove the solvent, diluted with dichloromethane (30 liters), and then K (15 ml) *. Extraction (30 ml) of hydrazine hydrochloride (30 ml) and mixed with water (10 liters) of hydrazine hydrochloride, dried on sodium sulfate, and shrunk under reduced pressure, to form an allyl ether intermediate ( 1 = 0.42 to a few (:, ethyl acetate / hexane, 10/90). For this allyl intermediate (2.5 4 g) in a solution of acetonitrile (25 liters), in 0¾ and nitrogen atmosphere Sodium hydrogen sulfide (252 g) was added. The resulting solution was warmed to RT »stirred for 16 hours, cooled to Ot: * Stop and add ammonium chloride aqueous solution to stop (15 ml) and concentrate to remove acetic acid * Re-diluted with MW water (30 liters) and extracted with dichloromethane (2 x 40 ml). The combined organic layers were washed with brine (15 ml), dried over sodium sulfate, and condensed under reduced pressure to yield the title compound. The physical properties are as follows: HMR (CDCla) 7.30, 7.21, 6.95, 6.86, 6.05, 5.41, 5.29, 4,82, 4.57, 2.59, 1.84, 0.95 3 ° Example 69 3- (1 ·-(2-allyloxy Phenyl) propyl) -4-hydroxymyristotin contains 4-hydroxycoumarin (337 mg), 1- (2-allyloxyphenyl) propionate (Preparation 36) (500 mg) in anhydrous Dibane (10 liters) In a flame-dried solution flask, boron trifluoride etherate (1.31 ml) was added under nitrogen. The resulting solution was stirred at RT for 25 hours, concentrated and the solvent was removed. Standard (CNS) 肀 4 specifications (210χ_29_7 mm) {谙 Read the precautions on the back before filling in this page). Binding. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A6 _B6___ V. Invention Description (128) Sodium Oxide Dilute the aqueous solution (5%, 20 mL) and extract with K2H2O2 (2x25 mL). The organic phase was discarded, and the aqueous phase M 6M hydrochloric acid was adjusted to be extracted with 1 * carbodimethane (2x25 ml). The organic phase was washed with brine (10 ml), dried over sodium acetate, and reduced under reduced pressure to produce a viscous residue, which was then chromatographed on a silica gel (230-40 0-pore sieve &gt; Hexane (5 / 95-10 / 90) gradient dissolution. MTLC was collected (ethyl acetate / hexane, 25/75) Rf = 0.44, and the solvent was removed to produce the title compound. The physical properties are as follows: Μρ 118- 120Ϊ: Prepare a solution of 37 1- (2-methoxyphenyl) propionate containing o-anisaldehyde (2.00 g) in anhydrous tetrachlorofuran (9.8 奄 L) in a flame-dried flask at 0¾ and A solution of ethylmagnesium bromide (3M diethyl ether, 5.4 ml) in anhydrous tetrahydrofuran (5.4 ml) was added under nitrogen, and the resulting mixture was stirred at 0¾ for 1 hour over 25 minutes. The saturated ammonium chloride was terminated (15 ml). ), And then separated. The aqueous layer was extracted with diethyl ether (2 X 30 ml), and the mixed layer was washed with brine (15 L), dried over anhydrous magnesium sulfate, and concentrated under pressure. Fengcheng oil was decanted on a silica gel (230-400 mesh sieve), and K-acetic acid / hexane (5 / 95-10 / 90) gradient dissolution. Pooled K TLC known (B Ethyl ester / hexane, 25/75) 1U = 0.44, and the solvent was removed to produce the title compound. The physical properties are as follows: _ MS (El) M * = 166.0998. Example 70 3- (1 *-(2- Methoxybenzyl) propyl) -4-hydroxycoumarin .............. ............................................. .......... Υ: .............. ^ (Please read the precautions on the back before digging into this page ) -130- This paper size is applicable to National Standards (CNS) A4 specifications (210X297 mm A A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention (3129) Follow the general steps of Example 67. Step, and there is no change in character, but the (2-methoxyphenyl) propionase of K 37 is substituted for the 1- (3-allyloxyphenyl) propionate, and it is obtained from diethyl ether / aqueous imitation The crude product was purified by recrystallization. • The title compound was obtained. The physical properties are as follows: Μρ 214-217Ό 〇 Preparation 39 1-bromo-1- (3-bromobenzyl) propane contains 1- (3-bromophenyl) Dry burn of Propionase (Preparation 38) (3.50 g) and Triethylamine (4.54 ml) in a solution of anhydrous diaerated methane (18 liters) , The Ot: and under nitrogen was added methane sulfonic Yong points Ml Dukes chloride (1.39 ml) "to generate the mixture was stirred at 0P 2 hours, K diluted with water (8 ml) was subdivided calendar. The leeches were extracted with dichloromethane (25 ml), washed with mixed organic calendar salt water (15 ml), dried over sodium sulfate, and concentrated under reduced pressure to form an oily intermediate. A mixture containing intermediates and lithium bromide (1.42 g) in propionate (50 ml), refluxed under nitrogen for 4 hours, cooled to RT. Concentrated, remove propionate, then dichloromethane (40 ml) and water (20 ml) Dilute * and tiller. The aqueous layer was extracted with dichloromethane (40 ml). The mixed organic layer was washed with brine (15 ml), dried over sodium sulfate, and condensed to form a crude oil, which was then decanted on silica gel (70-230 holes) (Sieve, 250 g) and dissolved with ethyl acetate / hexane (5/95). Pooling KTLC (ethyl acetate / hexane, 25/75) fractions of 1U = 0.63, and removing the solvent under reduced pressure can produce the title compound. 〇 Physical properties are as follows: MS (El) = 275.9143. {Please read the precautions on the back before filling in the nested pages} Loading, OK. -131- This paper size is used in China Guodong Coupling Standard (CNS) A4 Specification (210X 297mm i No. 83100S44 Patent Application Chinese) Revised instruction sheet (August 85) = B7 V. Invention description (\ 士 3) Example of printing by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 71 3- (1 '-(3-bromophenyl) propyl)- 4-hydroxycoumarin 4-hydroxycoumarin U98 mg) and bromo-1- (3-bromophenyl) propane (Preparation 39) (3.08 g) in a vial with a screw cap under nitrogen, and Place in 10010 oil bath. The mixture was heated to 175¾ at about 45 minutes, and the resulting melt was stirred at this temperature for 45 minutes, cooled to RT, diluted with M dichloromethane (45 ml), washed with water and brine (10 ml each), and sulfuric acid It was dried over sodium sulfate, and reduced to a residue under reduced pressure. The residue was chromatographed on silica gel (230-400 mesh sieve, 350 g), and dissolved in a gradient of ethyl acetate / hexane U5 / 85-60 / 40). The W TLC was pooled (ethyl acetate / curtin * 50/50) with fractions of Rf = 0.20 and the solvent was removed to give the title compound. The physical properties are as follows: Mp 168-172t :. Preparation 40 1- (4-Ethyloxyphenyl) propyl acetate (formula H-2) is shown in Figure Η. 1- (4-hydroxyphenyl) propionate (400 mg) in acetic anhydride (2 ml) The solution was added with pyridine (0.45 ml) under nitrogen. The solution was stirred at 01C for 30 minutes, then at RT for 2.5 hours, and then added to 1M hydrochloric acid (10 ml). The mixture M was extracted with dichloromethane (2 X 20 ml), and the mixed organic layer M was washed with brine (10 ml), dried over sodium sulfate, and concentrated under reduced pressure to give the title compound. The physical properties are as follows: CHN: found: C, 65,95; Η, 6.75. Example 72 3- (1 ·-(4-Ethyloxyphenyl ·) propyl) -4-hydroxycoumarin (formula Η-3) is shown in Figure Η 4-hydroxycoumarin (125 mg) and Europium carbonate (5 52 mg) in anhydrous B __-132 -___ This paper size applies to the Chinese national standard (CNS> Α4 size (210X297 mm) (Please read the notes on the back before filling in this page). Packing · , Π line A6 _B6__ V. Description of the invention (131) Mixture of shoulder (2.5 ml) · reflux under nitrogen for 5 minutes, and then in the M30 furnace, M is divided into six parts of 1- (4-acetoxybenzyl acetate 1 ΜHCl (10) was treated with a solution of propyl propyl ester (Preparation 40) (400 mg) in anhydrous acetonitrile (1 ml). The resulting mixture was stirred at reflux for 3 hours, and left at RT for 2.6 days. Ml). The mixture was extracted with ethyl acetate (3x15 ml) *, and the mixed organic layer was dried over anhydrous magnesium sulfate, and concentrated to form a first solid residue, which was then analyzed on silica gel (230-400 sieve, 45g) was dissolved with ethyl acetate / hexane (20 / 80-50 / 50). Sleep set W TLC (ethyl acetate / hexane, 50/50 &gt; known 1 = 0.09 fractions, and minus ® Remove solvent formation down The title compound has the following physical properties: MS (El) tr = 338.1144. Preparation 41 A mixture of 1- (2-hydroxybenzyl) propionate platinum oxide (302 mg) in methanol (30 ml) under an atmosphere of hydrogen (balloon) Stir for 1 hour, and then treat with K2-hydroxyethylphenyl (2, 000 g). The mixture is stirred under hydrogen for 4 hours. The catalyst is removed in a quenching manner, and the quenching solution is concentrated under reduced pressure, and an oily residue can be formed. The material was analyzed by sand glue (230-40 0 holes · 200 g), and dissolved in a gradient of ethyl acetate / hexane (5/9 5-20 / 80). Pooled WTLC ethyl acetate / hexane 25 * 25/75) with a fraction of 0.41, and the solvent can be removed under reduced pressure to generate the title compound. _ Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs {Please read the precautions on the back before filling in the clothing pages ) .The physical properties of the device are as follows: __ MMR (CDCU) 8.04, 7.16, 6.92, 6.83, 473, 2.78, 1.86 · 0.95 δ 〇-133- This paper standard is applicable to China National Standard (CNS) A4 specification (210X297 mm) Printed by A6 __B6__ by the Central Government Bureau of the Ministry of Economic Affairs, Cooperative Cooperative Fifth, the description of the invention (132) Preparation of 42- (2-ethylglycosylbenzene acetate) ) Propyl esters follow the 40-general method, regardless of identity changes, but K 1- (2-hydroxyphenyl) propionase (Preparation 41) replaces 1- (4-hydroxyphenyl) propionate * to obtain the title compound . The physical properties are as follows: MS (ΕΙ) Η * = 236.1051 〇 Example 73 3- (1 '-(2-Ethyloxyphenyl) propyl) -4-hydroxycoumarin Follow the general method of Example 72 • No According to some changes, but (2-ethoxyloxyphenyl) propyl acetate instead of 1- (4-ethoxyloxybenzyl) propyl acetate was used to obtain the title compound. The physical properties are as follows: CHH: Found: C, 70.69; Η, 5.19 〇 Preparation 43 4- (3-phenyl-2-propynyloxy) -coumarin (formula 1-2) is shown in Figure I. A flame-dried flask with a nitrogen inlet introduced tetrahydrofuran (ml), 4-hydroxycoumarin (293 ml), 3-phenyl-2-propyne-propionase (332 μl), and Sanbenten (711 奄) G), and there is a flush of nitrogen. Boil the bottle and stir and cool to Ot :. Diethylphosphonium azadicarboxylate (427 µl) was added dropwise to tetramethylfuran (5 ml) in a reaction / flask. The mixture was stirred for 15 hours while warming gently to room temperature. The solvent was removed under reduced pressure to produce a brown residue. The residue was partitioned into dichloromethane (50 liters) and water (50 liters), separated by organic calendar, washed with K water (3 x 25 ml) and brine (25 ml), dried over sodium sulfate, and reduced Scrape and concentrate M to form a bright yellow residue. It is chromatographed on a silica gel (230-400 mesh sieve, 75 g) and dissolved in hexane / hexyl acetate (90/10). Mixed flow confluence / (Rf = 0.35, TLC, hexane / acetic acid &lt; Please read the "Cautions on the back side", and then go to this page} -134- This paper size uses China National Standard (CNS) A4 specifications ( 210X297 mm _) _ A6 B6 Printed by the Central Bureau of the Ministry of Economic Affairs, Shellfish Consumer Cooperative, V. Description of the invention (133) Ethyl ester, 75/25) and shrinking M to generate the title compound. The physical properties are as follows: Mp 142-1461 ° Preparation 44 4- (2-3-phenyl-2-propenyloxy) -coumarin (formula 1-3) see Figure I Linda's catalyst (1 ^ 11 (1131 * '3) (8 g) were added to prepare 43 4- (3-phenyl-2-propynyloxycoumarin (200 mg), freshly distilled dichloromethane (14 liters) in acetic acid In a solution of ethyl acetate (20 ml). The mixture was sown for 4 hours under a hydrogen atmosphere (50 psi). The mixture was filtered through a celery disk, and the filtrate was concentrated and reduced to form a light butter. 400 mesh sieve, 75 g), hexane / ethyl acetate (95/5), dissolve. Mix the appropriate fractions (Rr = 0.46, TLC, hexane / ethyl acetate, 75/25), and concentrate K to form The title compound has the following physical properties: Mp 130-132¾ ° Example 74 4-hydroxy-3- (1-phenyl-2-propenyl) -coumarin (formula 1-4) See Figure I In a tube-flame dry flask, add 44- (Z-3-phenyl-2-propenyloxy) -coumarin (83 mg) to ortho-dimethylbenzyl. Soak the bottle in an oil bath. And preheated to 145t: The solution was refluxed for 36 minutes, and the flask was removed from the bath. It turned into a yellow solid residue, which was chromatographed on silica gel (70-230 mesh sieve, 100 g), mixed with M hexane / ethyl acetate (50/50). Mix appropriate fractions (Rf = 0.16, TLC, hexane / ethyl acetate 50/50) and concentrated to produce the title compound. -135- This paper size is applicable to National Standards (CNS) A4 specifications (210X297 mm) (Please read the precautions on the back before reading) Fill out this page} .. 馨 ：. 装 A6 ___B6__ 'V. Description of the invention (134) The physical characteristics are as follows:

Mp 127-1331C :. Example 75 4-Hydroxy-3- (5-6,7,8,9-tetrahydro-5H-benzocycloheptenyl) _ Coumarin on a flame-dried flask equipped with a nitrogen inlet, added under nitrogen 6,7, 8,9-tetrahydro-5H-benzocycloheptene-5-enzyme (500 g), 4-hydroxycoumarin (399 g) in anhydrous dioxane (20 l) And boron trifluoride ether acid (1.51 liters). The mixture was stirred for 4 hours, concentrated under reduced pressure, diluted with sodium hydroxide (10% * 10 liters), and extracted with dimethyl dichloromethane (3x50 liters). The organic extracts were mixed, washed with M saline (10 liters), dried over sodium sulfate, concentrated under reduced pressure, and chromatographed on silica gel (70-230 mesh sieve, 75 g). 5). Mix the appropriate fractions and reduce pressure to produce the title compound. The physical characteristics are as follows:

Mp 183-1851C ° Example 76 4-Ethyl-3- (1- (6-methoxy) -1,2,3,4-tetrahydronaphthyl) -coumarin Follow the general method of Example 75, and There is no phenotypic change, but M 1,2,2. &Lt; 3,4-tetrahydro-6-methoxy-1-naphthalene (692 g) instead of 6,7,8,9-tetrahydro -5'-Benzenecyclohepten-5-ol to give the title compound. The physical characteristics are as follows: Printed by Behr Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs (please read the precautions on the back before filling in this page)

Mp 90-95 ¾ ° _ Example 77 4-hydroxy-3- (1- (7-methoxy) -1,2,3,4-tetrahydronaphthyl) · Coumarin-136- _ This paper size Applicable to National Standard (CNS) A4 specifications (210X297 mm) A6 B6 Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention U35) Follow Example 75-General steps * No critical changes, but Ml , 2,3,4-tetrahydro-7-methoxy-binaphthalene (69 2 g) instead of 6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol, but The title compound was obtained. The physical properties are as follows: Μρ 95-100Ό ° 78 Example 78-106 Using similar procedures as described above, the following additional compounds of the present invention (some of which are shown in the mass spectral data of Table I below) can be prepared: 78) Myristole * 7- (allyloxy) -3- (ot -ethylbenzyl) -4-hydroxy- 79) coumarin, 3- [ct -ethylearm-3-yl) ethyl] carbonyl] Amine] benzyl] -4-hydroxy-80) coumarin, 3- [bis (cyclopropyl) methyl] -4-hydroxy-7-methoxy 81) myristotin, 3-U-ethyl Benzyl) -4-hydroxy-7- (1-methylethoxy) -82) coumarin, 7-ethoxy-3-U-ethylbenzyl) -4-hydroxy-83) butyl Acid, 2- (4-physyl-'2-isopropyl-21 ^ 1-benzopyridin-3-yl), ethyl ester 84) coumarin, 4-hydroxy-3- (2-benzidine Group)-85) Coumarin, 4-hydroxy-3- [l- (4-hydroxybenzyl) propyl]-86) Coumarin * 7-trifluoromethyl_yl-4-hydroxy-3-U -Phenylpropyl)-87) Coumarin, 6-fluoro-4-hydroxy-3- (1-phenylpropyl)-88) Myristotin · 4-hydroxy-7-methoxy-3- (1-phenylpropyl)-(谙 Please read the precautions on the back before filling in this page. I. Binding.-Thread. Specifications (210X297mm) Printed Chinese Manual of Patent Application No. 83100644 by the Consumer Standards Cooperative of the Ministry of Economic Affairs (August 85) A7 B7 V. Description of the Invention (89) Coumarin, 4-hydroxy-6 -Methoxy-3- (1-phenylpropyl) -90) coumarin, 4-hydroxy-7-methyl-3-U-benzylpropyl) -91) myristotin * 3- [ 1- (4-bromophenyl) propyl] -4-hydroxy-; Mp: 188.5-191T: 92) Coumarin, 7-chloro-4-hydroxy-3- (1-phenylpropyl) -93 ) Coumarin, 4,7-dihydroxy-3- (1-phenylpropyl)-94) Coumarin, 4-hydroxy-3- [1- (4-methoxyphenyl) propyl] -;

Mp: 149-15110 02 ... 95) Coumarin, 4,6-dihydroxy-3- (1-phenylpropyl) -96) Coumarin, 6-amino-4-hydroxyl: 3- (1-phenylpropyl) -97) coumarin, 4-hydroxy-3- [1- (3-methylphenyl) butyl]-98) coumarin, 3- [1- (3- Cyanophenyl) propyl] -4-hydroxy-99) 2N-naphtho [1,2-b] piperan-2-one, 4-hydroxy-3- (1-phenylpropyl) -100) Coumarin * 4-hydroxy-3- [l- [4- (2,3-dihydroxy) propoxybenzyl] propyl] -101) Coumarin, 3- [1- (3-cyanobenzene Group) ethyl] -4-hydroxy-102) coumarin, 4-hydroxy-3- [1- (3-methoxyphenyl) propyl]-; Mp: 141-143.5 ^ 103) coumarin , 4-hydroxy-3- [1- (3-hydroxyphenyl) propyl] -104) 3- (dicyclopropyl) methyl-4-hydroxycoumarin 105) 4-hydroxy-3- (1 -Phenylpropyl} -coumarin 106) Coumarin, 4-hydroxy-3- [1- (4-propanylphenyl) propyl]-Example 107 3- (Cyclopropylphenylmethyl) -5,6,7, δ, 9, 10 -Hexahydro- 4- ._- 138 -_ This paper adopts China National Standard (CNS) Α4 specification (210 × 29? Mm) (Please read the note on the back first (Please fill in this page for further information.) Chinese Specification for Patent Application No. 83100644 Front page (August 1985) A7 B7 V. Description of invention (\ V /) Printed hydroxyl-2h-cyclooctane [b] uran-2-one (Formula J-3, Where h is cyclopropyl, dagger is benzyl, and η is 4> (also formula L-1, where η is 4, and 1 is cyclopropyl). See Figure κ and L for 50 ml with 10 ml pressure balance. Liquid funnel (filled with 3A activated molecular sieves) and a three-necked round bottom flask with a reflux condenser and a nitrogen inlet, filled with cyclooctene-acrylic acid, Ling, 2-dihydroxylactone (0.753 g), para- Toluenesulfonic acid (0.184 g) and 10 ml of toluene. Add -cyclopropylbenzyl alcohol (0.55 ml) and warm the reaction mixture to about 1 40 π. Add after 2.5 hours and 5 hours Λ additional α-cyclopropylbenzyl alcohol (0.37 ml). After a total of 7 hours * the reaction mixture was diluted with 100 ml of 1N sodium hydroxide and washed with 50 ml portions of ether. The aqueous layer was concentrated with concentrated hydrochloric acid. Adjust from 14 to 1. A white precipitate can be formed, and two 50 ml portions of dichloromethane are extracted. The organic (dichloromethane) layer is mixed again, dried over magnesium sulfate, dried and concentrated to obtain a white precipitate. . To 1.128 g white solid was 50 g silica gel column chromatography upstream tube, (Μ 20% ethyl acetate - hexyl eluting hospital) may generate 0.859 g of the title product as a white solid. The physical properties are as follows: Μρ 173.8-175. ° HMR (CDC13) 5 7.51, 7.38, 7.28, 6.26, 3.99, 2.62, 2.44, 1.80-1.72, 1.60-1.32, 0.78-0.70, 0.64 -0.56, 0.32-0.26 ρρβι〇 -13C HMR (CDC13) S 3.71, 4. · 81, 13.06, 22.03, 25.75, 26.17, 28.77, 29.13, 30.63, 43.63, 106.19, Π0.66, 127.31, 127.84, 129.09, 140.93, 161.21, _- 139- __ This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm> ~~ (Please read the notes on the back first, and then fill in this page)-installed., Ιτ 线 83100644Patent application Revised page of Chinese manual (August 85) A7 B7 V. Description of invention (d $) 163.97, 165,68 ppb〇IR (Nujol) 3155, 3080, 2954, 2921, 2852, 1665, 1559, 1407, 1190, 1182 , 1172, 706 cm-1. Measured value of elemental analysis: C, 77.90; Thallium, 7.68. MS (El) m / e 324, 296, 295, 283, 233, 207, 131, 91 〇Spring example 108-117 Use The above steps can prepare + other compounds of the present invention under K: 108) 5,6,7,8,9,10-hexahydro-4-hydroxy-3- (1-phenylpropyl) -2Η-cyclooctyl [ b] 那 -2--2- (Formula J-3, R is ethyl, R2 is phenyl »η is 4) See figure J. Physical properties are as follows: 0.40 4 g of the title product was isolated as a white solid. Ηρ 188‘9-190.6t !. &quot; H HHR (CDC13) S 7.44-7.35, 7.30.7.24, 5.76, 4.37, 2.63-2.59, 2.42-2.37, 2.21-1.98, 1.77-1.71, 1.53-1.38, 1.02ppo. 13C HMR (CDC13) 5 165.5, 163.8, 161.2, 141.5, 129.3, 127.5, 127.2, 110.5, 106.2, 41.2, 30.6, 29.1, 28.8, 26.1, 25.7, 23.9, 22.0, 12.2 ppm. IR (Huiol) 3174, 2954, 2924, 2868, 2853, 1664, 1640, 1566, 1462, 1447, 1410 ^ 1188, 1172, 1114, 1101, 1057, 61 1 cm. Elemental analysis found: C, 76.58; H, 7.66. -140-This paper size is applicable to China National Standard (CNS) A4 specification (210 ×: 297 mm) Printed on the Chinese Manual for Patent Application No. 83100644 by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) A7 B7_ V. Description of the invention (ίφ MS (El) ® / e 312, 297, 283, 255, 221, 153, 91. The measured value of the high-resolution spring: 312.1721. 109) 5,6,7,8-tetrahydro 4-Hydroxy-3- (1-phenylpropylbenzopiperan-2-fluorene (formula L-1 * where η is 2 and 1U is ethyl) see Figure L. The physical properties are as follows. 0.549 is isolated Gram of the title product as a white solid. Μρ 177. 5-179 H-XW NMR (CDC13) 5 7.45-7.35, 7.30-7.25, 5.76, 4.35, 2.48, 2.24-2.20, 2.18-1.99, 1.81-1.70, 1.69 -1.63, 1.03 ppm ° 13C NMR (CDCU) 5 165.03, 163.9, 158.4, 141.8, 129.2, 127.5, 127.1, 108.4, 106.0, 41.2, 27.1, 23.9, 21.5, 21.4, 20.2, 12.3 ppm〇IR (Nujol) 3156 , 3085, 3058, 3025, 2954, 2926, 2870, 2856, 1668, 1634, 1559, 1460, 1451, 1430, 1404, 1377, 1216, 1182, 1153, 1117, 1107, 1090, 756, 699 cm_1. Elemental analysis found: C, 75.79; H, 7.05 MS (El) m / z 284, 269, 255, 227, 131, 125, 91. 110) 6,7,8,9-tetrahydro-4-hydroxyphenylpropyl) -cyclohepta [b] piran -2 (5H) _ 詷 r The physical properties are as follows: 0.172 g of the title product of a 圼 white solid was isolated. -141-This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm) I ------------ Installation ------ Order ----- J 丨 Line ( Please read the note on the back ^ bird and fill in ^ this page) No. 83100644 Patent Application Chinese Manual Correction Page (August 1985) A7 B7 V. Invention Description UA) Printed by the Consumers' Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs p 7 2-7 5 t: (decomposed). αΗ HMR (CDC13) S 7.44-7.36, 7.31-7.26, 5.84, 4.38, 2.71-2.67, 2.42-2.38, 2.23-1.96, 1.77-1.73, 1.70-1.62, 1.56-1.49, 1.3 ppm® 13CNHR (CDC13) 5 165.0, 163.8, 141.5, 129.4, 127.5, 127.3, 113.1, 105.6, 41.2, 33.8, 31.3, 26. 1, 24.4, 23.8, 22.1, 12.2 ppm. IR (Hujol) 3126, 3085, 3058, -3025, 2954, 2922, 2869, 2855, 1657, 1627, 1602, 1548, 1494, 1453, 1434, 1406, 1377, 1266, 1225: 1194, 1154, 759, 6 9 9 cm-1. Elemental analysis found: C, 76.22; Η, 7.67. MS (El) m / z 298, 269, 242, 139, 119 ° 111) 6,7-dihydro-4-hydroxy-3-U-phenylpropyl) -cyclopentyl [b] piperan-2 The physical properties of (5H) -one are as follows: 0.285 g of the title product of a pale yellow solid is isolated. Mp 183.4-1 85.6t: ° NHR (CDC13) 5 7.43, 7.34, 7.24, 6.29, 4.30, 2.76, 2.62-2.57, 2.22-2.00, 1.00 ppm 〇13C NMR (CDCU) δ 166.7, 163.6, 163.2, 142, 2, 129.0, 127.6, 126, 9, 111.3, i04. 9,41.7, 31.1, 25.4, 23.9, 19.8, 12.4 ppm 0 IR (Hujol) 3079, 3056, 3022, 2956, 2925, 2871, -142- ----------- ^-I (please read the note on the back # ^ before filling in «this page) The size of the paper on this guideline applies the Chinese National Standard (CNS) grid (210X297 mm) Economy The Ministry of Standards and Technology Bureau's Work Cooperative Consumers Co., Ltd. printed a revised page of the Chinese specification for patent application No. 83100644 (δmonth of 1985.) Α7 __ Β7 V. Description of the invention (10 2855, 1672, 1662, 1627, 1561, 1461, 1448 , 1436, 1425, 1377, 1245, 700 cm_1. Measured values of elemental analysis: C, 75.37; H, 6.65 ° MS (El) η / ζ 270, 241, 213, 153, 111, 91. 112) 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-cyclohepta [b] piperan-2 (5H) -one (formula L-1, wherein η is 3, h is cyclopropyl) See L diagram. The physical properties are as follows:… 0.896 g (69%) of the title product was isolated as a white solid. Mp85-88t: (decomposed). _ ^ HHR (CDC13) 5 7.52, 7.37, 7.28, 6.24, 3.97, 2.70, 2.47-2.43, 1.82-1.75, 1.71-1.64, 1.59-1.52, 1.37-1.29, 0.78-0.71, 0.65-0.57, 0.32-0.26 ppb «13C HMR (CDC13) S 165.3, 163.9, 163.8, 140.9, 129.1, 127.9, 127.4, 113.2, 105.7, 43.7, 33.8, 31.3, 26.1, 24.4, 22..1, 1 3.0, 4.9, 3.8 ppm ° IR (Nujol) 3138, 3076, 3060, 3025, 2997, 2952, 2923, 2868, 2855, 1658, 1628, 1549, 1495, 1455, 1433, 1406, 1377, 1275, 1228, 1196, 1154, 1138, 1071, 1067 , 704 cm-1. Elemental analysis found: C, 77.03; H, 7.18. MS (El) ni / z 31 0, 282, 281, ^ 269,219, 1 31, 91 〇 Measured value at high resolution: 310. 1578. 113) 3- (Cyclopropylbenzylmethyl) -6,7-dihydro-4-hydroxy-cyclopenta [b] piperidine __- 143 -_ This paper size applies to China National Standard (CNS) A4 (210X297 mm) ------- ^-1--install ------ order ---- 1 line (please read the notes on the back ^ before filling this page) page 83 100644 Revised Page of Chinese Specification for Patent Application No. (August 1985) ^ V. Description of the Invention (Nan-2 (5Η)) The physical properties are as follows: 0.695 g of the title product is isolated as a white solid. Μ ρ 1 8 3.3 -18 4.81: 〇αΗ NMR (CDC13) 5 7.50, 7.35, 7.26, 6.51, 3.84, 2. 77, 2.60, 2.05, 1. 51-1.40, 0.78- 0.70, 0.69- 0. 49, 0.31- 0.23 ppm c &gt; 13C HHR (CDCla) δ 166. 9, 163, 6, 163.3, 141.6, 128.9, 127. 8, 127 Ill .5, 105.1, 44.3, 31.1, 25 .5, 19.8, 13.0, 5. 1, 3 .8 ρ ρ in 0 IR (Hujol) 3001, 2955, 2924, 2867, 28.56, 1661, 1612, 1566, 1544, 1439, 1424, 1375, 1261, 1223 cm-1. (Please read the precautions on the back # ' (See this page).

.1T Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economics Measured value of elemental analysis: C, 76.21; Η, 6.33. MS (El) b &gt; / z 282,253, 241, 165, 131, 111, 91 〇114) 3- (cyclopropylphenylmethyl) -5,6,7,8,9,10,11, 12,13,14 -Decahydro-4-hydroxy-2H-cyclododecane [b] piperan-2-_ Physical properties are as follows: 0.2 45 g of the title product Mp 97.8-99 as a white solid was isolated. Ot: ° αΗ NMR (CDC13) 5 7.51, 7.37, 7.29, 6.20, 3.97, 2.55-2.49, 2.32, 1.88-1.83, 57-1.50, 1.40-1.33, 1.31-1.23, 0.77-0.70, 0.65-0.58, 0.32-0.26 ppb〇13C NHR (CDCla) ^ 165.3, 164.7, 160.7, 140.9, -144-The size of thread paper is applicable to the Chinese National Standard (CNS) A4g (210X297 mm) No. 83100644 Amendment page of the Chinese specification of patent application (8,85 Month) A7 V. Invention Description (f4) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economy 129.1, 127.9, 127.4, 111.7, 106.4, 43.6, 27.5, 26.8, 25.0, 24.9, 24.8, 23.7, 22.5, 22.1, 21.9, 14.0, 13.0, 4 · 9, 3.9ρρ®0 IR (Hujol) 2942, 2923, 2855, 1658, 1632, 1546, 1468, 1208 cm-1. Elemental analysis found: C, 78.93; Η, 8.48. MS (El) m / z 380, 352, 339, 289, 131. 115) 3- (cyclopropylphenylmethyl) -5,6,7,8-tetrahydro-4-hydroxy-2H-1-benzopiperan-2-one Mp 180 · 0-181.2t :. … ΑΗ NHR (CDC13) § 7.52, 7.35, 7.26, 6.14, 3.92, 2.49, 2.30-2.26, 1.82-1.74, 1.72-1.65, 1.40-1.31, 0.79-0.70, 0.63-0.56, 0.32-0.24 ppm ° 13C NMR (CDCU) 5 165.3, 163.9, 158.4, 141.2, 129.1, 127.8, 127.3, 108.6, 106.1, 43.7, 27.1, 21.6, 21.4, 20.2, 13.0, 5.0, 3.8 ppm. IR (Hujol) 3025, 2996, 2952, 2924, 2867, 2855, 1668, 1634, 1564, 1460, 1450, 1407, 1377, 1219, 1 1 81, 7 0 5 cm-1. Elemental analysis found: C, 76.99; Η, 6.96. MS (El) ffl / z 298, 268, 179, -131〇116) 3- (cyclopropylphenylmethyl) -5,6t7,8,9,10,11,12-octahydro-4-hydroxy -The physical properties of 2H-cyclodecyl [b] piperan-2- 嗣 are as follows: 145-This paper size is in accordance with Chinese National Standard (CNS) A4 specification (210X297 mm) Please read the notes on the back first and then fill in a page. The staffing cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed the Chinese specification for the patent application No. 83100644 amendment page (August 85) A7 B7 V. Description of the invention (/ ^ 0.315 g of the title product of white solid was isolated.

Mp 87.6-90.4¾. aH HHR (CDC13) 5 7.51, 7.38, 7.28, 6.20, 4.02, 2.74-2.68, 2.50, 1.88-1.84, 1.67-1.57, 1.45-1.40, 1.38-1.31, 1.29-1.21, 0.77-0.71, 0.67-0.56, 0.33-0.27 ppm ° 13C NHR (CDC13) 5 165.5, 164.6, 160.3, 140.8, 129.1, 127.8, 127.4, 111.1, 106.2, 43.4, 28.8, 26.9, 25.7, 25.4, 25.3, 22.7, 33.5, 21.1, 20.7, 13.0 , 4.8, 3.6ppmo IR (Hujol) 3076, 3024, 2998, 2929, 2856, 2857, 1660, 1632, 1547, 1455, 1449, 1396, 1230, 1206, 1193, 1171, 1130, 696 cm-1. Elemental analysis measured value · C, 78.41; Η, 8.12. M S (Ε I) in / ζ 3 5 2, 3 2 4, 3 1 1, 2 6 1, 2 3 4, 1 31. Measured value at high resolution: 352.2038. 117) 3- (cyclopropylphenylmethyl) -6,7,8,9,10,11-hexahydro-4-hydroxy-cyclonon [b] piperan-2 (5H) The physical properties are as follows: 0.194 g of the title product was obtained as a white solid.

Mp 81. 7-84.0T :. -XH HMR (CDC13) 6 7.51, 7.37, 7.29, 6.22, 4.01, 2.65-2.61, 2.46-2.43, 1.79-1.78, 1.58-1.31, 0.79-0.70, 0.66-0.57, 0.33-0.25 ppm 〇-146-this Paper size applies to Chinese national standard (CNS> A4 specification (210X297mm) ---------- installation ------ order -------- V-line (please read the back first Note YA, please fill in this page again) Printed Patent Application No. 83100644 by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 修正 Chinese Manual Revised Page (August 85) A7 B7 V. Description of Invention (f β 13C NHR (CDC13) 5 165.6, 164.2, 161.1, 140.8, 129.1, 127.9, 127.4, 111.6, 106.3, 43.5, 30.2, 25.9, 25.7, 25.0, 24.9, 24.0, 22.9, 13.1, 4.8, 3.7 ppm ° IR (Hujol) 3133, 3075, 3060 , 3024, 2996, 2950, 2923, 2867, 2856, 1659, 1632, 1550, 1466, 1451, 1400, 1207, 1181, 1157, 1138, 700 cm-1. Measured values of element analysis ··, C, 77.47; ji, 7.59. MS (El) m / z 338, 310, 247, 221, 131, 91. Measured value at high resolution: 338.U72. &Lt; Example 118 3- (Dicyclopropylmethyl) -5,6, 7,8,9, 10-hexahydro-4-hydroxy-2H-cyclooctane [b] Niran-2- 嗣 (formula J-3, where iU Cyclopropyl, Cyclopropyl * η is 4) See figure J. A 50 ml addition funnel (filled with activated 3A molecular sieve) with a pressure balance of 10 ml, a reflux condenser and a three-necked nitrogen population A round bottom flask was charged with cyclooctene-butyl acrylic acid; 8,2-dihydroxy-δ-lactone (0.483 g), p-toluenesulfonic acid (0.118 g) and 2 ml of toluene. Dicyclopropylmethyl A solution of yeast (0.41 8 g) in 8 ml of toluene, and the reaction mixture was warmed to about 140 t: After 1 hour, more methanol (0.280 g) was added. After 2 hours of hydroxyl, the reaction mixture was κοοοmL It was diluted with sodium hydroxide and washed with two 50 ml portions of acetic acid. The pH of the aqueous layer was adjusted from 14 to 1 with concentrated hydrochloric acid. A white precipitate formed, which was extracted with three 50 ml portions of dichloromethane. The organic layer (dichloromethane) was mixed again, dried over magnesium sulfate, dried and concentrated to give 0.483 g of a white solid. At 50 grams of silicone ascending column __; _-147-This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the note on the back before completing this page) ---- 1 ----------- Binding d .------- Patent Application No. 83100644 Revised Chinese Manual (August 85) A7 V. Description of Invention (/ Staff of Central Bureau of Standards, Ministry of Economic Affairs Chromatography printed by a consumer cooperative (dissolved with 2096-30% acetic acid acetate-hexane) produced 0.3341 g of the title product as a white solid. The physical properties are as follows: Mp 196.9-197. 5 ¾ ° NMR (CDC13) 5 7.44, 2.68, 2.64-2.60, 2.56- 2.52, 1.79-1.71, 1.69-1-61, 1.55-1.41, 1.04-0.93, 0.60-0.51, 0.48-0.42 ppm ° 13C NMR (CDCl3) 5 165.7, 164.3, 160.8 , 110.4, 105.4, 39.7, 30.6, 29.2, 28.8, 26.2, 26.0, 22.1, 12.4, 3.6, 2.4ppm ° IR (Nujol) 3078, 3008, 2996, 2954, 2926, 2856, 1658, 1610, 1547, 1413, 1235, 1215, 1205, .1176, 1160, 1 102, 1 179 cm-1. MS (El) m / z 288, 260, 259, 247, 232, 950 is measured at high resolution. · 28δ. 1731. Example 119 Aminocarboxylic acid, [3- [cyclopropyl (5,6,7 , 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-* phenylmethyl ester (Formula M- 6) See Figure M. A 12 liter three-necked round bottom flask with a Soxhlet extractor (containing 3A molecular sieve (180 g)) and a nitrogen inlet was filled with human cyclooctene-acrylic acid, / 3,2-dihydroxy -δ-lactone (59.6 g), p-toluenesulfonic acid (14.9 g) and dichloromethane (7.2 liters). Cyclopropyl- (3-aminobenzyl) prepared as described in r in Preparation 49-52 Ester-benzyl) methanol (90.00 g) was added, and the reaction mixture was warmed to reflux for 1 hour. The reaction mixture was cooled to 200 t), and saturated with M 1: 1 ___- 148 -______ This paper size applies Chinese National Standard (CNS) Α4 Specification (210 × 297 mm) (Please read the precautions on the back before filling this page) • Binding · Binding-Thread {ιη) No. 83100644 Patent Application for Chinese Manual Amendment Page (1985) Month> A7, B7 V. Description of the invention Wash with sodium chloride / saturated sodium bicarbonate (3 liters), water (3 liters) and saturated sodium chloride (3 liters), κ methylene chloride backwash each aqueous layer (2 X 1.5 liters). The organic layers were remixed, dried over sulfuric acid, filtered, and concentrated to about 1.5 liters. The reaction mixture was cooled to -20 t: over 72 hours, filtered, and dried under reduced pressure to yield 103.5 g. The crude product was re-slurried with 12.5 ml / g hexane and dried to yield 102.4 g of the title compound. The mother liquor was reduced from recrystallization and the residue was recrystallized from ethyl acetate to obtain another 10.9 g of the title compound. The physical properties of the title compound are shown in Example 11 9A. Example 119A Aminocarboxylic acid, [3- [cyclopropylli (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- Group) methyl] benzyl]-, phenylmethyl ester, (formula J-3, where 1U is cyclopropyl * Rz is meta- (HHC〇2_ benzyl) phenyl, η is 4). (Also Formula K-1) See J and K diagrams. In a 50-ml three-necked round-bottomed flask with a reflux condenser and a nitrogen inlet, add cyclooctene-butyl acrylic acid, 2-dihydroxy-δ-lactone (0.299 g), and para-methanesulfonic acid (0.053). G) and 3A molecular sieves. Cyclopropyl- (3-aminobenzyl phenyl) methanol (0.300 g) prepared as described in Preparation 45-47 was added to a solution of 5 ml of toluene, and the reaction mixture was warmed to 110.0 ° C for 7 hours. The reaction mixture was diluted with 50 ml of 1H sodium hydroxide and washed with two 25 ml portions of acetamidine. The pH of the aqueous layer was adjusted from 14 to 1. A white precipitate formed, which was extracted with three 50 ml portions of dichloromethane. The organic (dichloroformamidine) layers were remixed, dried over magnesium sulfate, dried, and concentrated to yield 0.275 g of a white-brown solid. Chromatography on a 20 g silica gel column (35-100% B, 149) This paper is in accordance with the Chinese National Standard (CNS) A4 specification (210X297 mm) ---------- Yiyi ---- --1T ---- 'I 1'. '(Please read the notes on the back of the iodine and then fill out 1 page) Dumpling printing by the Central Bureau of Standards, Ministry of Economic Affairs, printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs 83100644 Patent Application Chinese Specification Correction Page (March 85) A7 B7 V. Description of the Invention (ίβ) Ether-hexane and subsequent 5% methanol-dichloromethane dissolution) can produce 0.46 g of the title product as white Solid, and a mixture of 0.176 g of the title product and the starting piperanone. The physical properties are as follows: 113-1151 ° (decomposed). M NMR (CDC13) 5 7.48, 7.38-7.26, 7.17, 6.70, 6.29, 5.20, 3.95, 2.64-2.60, 2.47-2.43, 1.76-1.72, 1.6, 1.42, 0.88, 0.73--0, 72, 0.63-0.55 , 0.29-0.26 ρριβ ° 13C NMR (CDC13) δ 165.6, 1-64.0 '161.3, 142.2, 138.5, 129.9, 128.5, 128.3, 128.2, 122.9, 118.0, 117.9, 117.6, 110.7, 106.0, 67.0, 43.7, 30.7, 29.1, 28.8, 26.2, 25.8, 22.1, 13.0, 4.9, 3.8 ρρβι ° IR (Hujol) 3304, 2995, 2953, 2923, 2855, 1734, 1698, 1665, 1666, 1633, 1610, 1595, 1553, 1491, 1463 , 1455, 1445, 1406, 1 377, 1313, 1222, 1175, 1085, 1068, 740, 696 cm-1 ο MS (ED m / z 473, 445, 382, 338, 91 〇 measured values at high resolution: 473.2202. Example 120 1 (3- (Cyclopropyl- (4-hydroxy-2-oxy-5,6,7,8,9, 10-hexahydro-2H-cyclooctane [b] pulsan-3- (Methyl) -methyl) -phenyl) -N ', fluorene "-diisopropyl legs (Formula K-3) See Figure K. A barium hydrogenation tube was added with fluorene :: (: (0.02 4 g), example 1196 standard __; _- 150 -_ This paper size applies to Chinese national standards (CNS &gt; Α4 size (210X297 mm) ---------- installation ---- --Order one ----- rr \ —— line I: v. (Please read the notes on the back before filling-^ this page) Printed by A6 __; _ '_B6 of the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 2. Description of the invention (149) The title product (Formula Kl) (0.133 g) and 2 liters of methanol. The tube was shaken at 40 psi hydrogen and room temperature for 20 hours. The reaction mixture was diluted with formazan and filtered through a plug. And concentrated M to produce 0.120 g of the compound of formula K-2 (as a white solid) 'It can be used directly without further purification (HS (El) m / z 339, 31 1, 310 · 213, 187, 159). A Burmese 10 ml bottle with hydrogen and two necks, filled with human 1:-&amp; 〇 &lt;1-; 3-alanine (0.064 g), a compound of formula 1 [-2 (0.120 g), and 1 liter Digas methane. 3-Diisopropylcarbodiimide (0.044 ml) was added dropwise, and the reaction mixture was stirred at room temperature for 4 days. The reaction mixture was concentrated K to give 0.300 g of rose oil. An analysis of the 25 g silicone ascending column can produce 0.080 g of the title product, which is a light rose solid film. 〇 The physical properties are as follows:

Mp 172-175 1C (decomposed). τΗ NMR (CDC13) 5 7.40, 7.23, 7.19, 6.97, 6.74, 3.92-3.85, 3.72, 3.48, 1.76-1.68, 1.42-1.26, 1.21 -1.18, 0.91-0.86, 0.62-0.70, 0.42- 0.51, 0.37- 0.36 ppm ° 13C NMR (CDCla) δ 165.7, .160.4, 153.7, 150.5,

• 'I 146.4, 134.8, 129.6, 129.2, 126.6, 123.7, 121.6, 112.3, 105.7, 45.7, 30.8, 29.3, 28.9, 28.3, 26.2, 25.9, 22.4, 13.9, 12.7, 6.2, 3.9 ppb ° IR (Nujoi) 3073, 305δ, 2952, 2921, 2868, 2854, 1658, 1637, 1619, 1588, 1589, 1488, 1461, 1445, 1425, 1389, 1368, 1353, 1334, 1171, 1128 cm-1. -151- This paper uses China National Standards (CNS) A4 specifications (21 × 297 mm) (Please read the precautions on the back before filling out this page) • • -rs · • No. 83100644 Patent Application Revised Chinese Manual (August 85) A7 B7 V. Description of Invention (ί β MS (El) 465, 379, 339, 310, 277, 233, 187, 146, 130, 119, 85, 69, 58, 44 m / z ® Example 121 10-cyclopropylmethyl-3- (cyclopropyl-phenylmethyl) -4-hydroxy-5,6,7, δ, 9,10-hexahydro-cyclooctyl [ b] piperan-2-one (Formula L-2, where [^ is cyclopropyl * 1 ^ 2 is-(:}] 2 •• cyclopropyl, η is 4) see L chart. Central Standard of the Ministry of Economic Affairs Bureau ’s Consumer Cooperative printed a 50-ml three-necked round-bottom flask with a nitrogen inlet and a 10-ml pressure-equipped addition funnel * Diisopropylamine (0.25 ml) and 2 ml of tetrahydrofuran were added to the addition funnel. A solution of the title product of Example 107 (0.29 g) in 4 ml of tetrahydrofuran. The flask was placed in an ice bath, and human n-butyllithium (1.10 ml) was added dropwise over a period of 2 minutes. After stirring for 20 minutes at 0.00 The reaction was cooled to -401 in a dry ice / propane bath: * And the solution of the title product of Example 107 was added dropwise over 5 minutes. The addition funnel K was wetted with 1 ml of tetrahydrofuran, and the fresh orange reaction mixture was stirred at -50 to -30 t for 20 minutes. Bromine was added dropwise during the M1 minute period. Methylcyclopropane (0.083 ml), the reaction mixture was stirred for 2.5 hours when warmed to 10P. The pale yellow solution was stopped with 10 ml of 10% hydrofluoric acid, and a small amount of sodium chloride was added. The reaction mixture was then added in two portions. Extracted with 30 ml of dichloromethane, dried over magnesium sulfate, filtered, and concentrated to produce 0.271 g of a white solid. Chromatography on 25 g of silica gel produced 0.32 g of the title product * as a white solid. The physical properties are as follows: -

Mp 86-90t: ° ^ αΗ NMR (CDC13) 5 7.51, 7.38, 7.30, 6.23, 4.01, 3.07-3.03, 2.78-2.73, 2.24-2.20, 2.02-1.94, 1.79- ______- 152 -_, paper size Applicable to China National Standard (CNS) A4 specification (21 OX297 mm) No. 831Q0644 Patent Application Chinese Manual Correction Page (August 1985) A7 B7 V. Invention Description (called) Economy, Ping Central Standards Bureau Staff Consumer Cooperatives System 1.56, 1.39-1.24, 1.21-1.14, 0.86-0.64, 0.63-0.58, 0.43-0.39, 0.32-0.27, 0.09-0.07 ppb. 13C HMR (CDC13) 5 165.5, 163.7, 162.4, 162., 3 141.0, 129.1, 127.9, 127.8, 127.3, 112.0, 105.9, 105 · 7, 43.6, 43.5, 39.5, 39.4, 36.2, 35.5, 30.4, 30.3, 27.2, 25.7, 25.6, 23.0, 13.1, 13.0, 9.6, 9.5, 4.9, 4.6, 4.4, 3 · 7, 3.6 ppm ° IR (Nujol) 3024, 2996, 295-3-,-2922, 2868, 2855, 1657 , 1631, 1545, 1460, 1455, 1402, 1209. 1197 ,. 11 7 9, 11 31 cm-1. — · Result of elemental analysis: C, 79.34; Η, 8.29. MS (El) m / z 378, 350, 349, 337, 287, 131, 91, 55 ° Examples 122-133 Other compounds of the present invention under K can be prepared by a method similar to the above 122) 10-benzyl-4 -Hydroxy-3-U-phenylpropyl-5,6,7,8,9,10-hexahydro-cyclooctane [b] piperan-2-one isolated 0.041 g of the title product as a white solid. The physical properties are as follows: Mp 76-80 C (decomposed). -^ HMR (CDC13) 6 7.40-7.30 «7.28-7.17, 5.77- 5.75, 4.40-4.35, 3.30-3.19, 2.88-2.81, 2.78-2.59, 2.21-1.94, 1.70-1.60, 1.33-1.23, 1.05-0.90 ppm〇-153-This paper size is in accordance with Chinese National Standard (CMS) A4 (210X 297mm) Please read the back © and fill in-write down ... Printed the revised Chinese specification of Patent Application No. 83100644 (August 85) A7 B7 V. Description of the invention (ey 13C HMR (CDCls) δ 140.1, 129.4, 128.9, 128.3, 128.2, 128.0, 127.5, 127.4, 127.3, 126.0, 41.0, 40.9, 37.3, 37.2, 35.2, 30.2, 27.0, 25.6, 23.9, 22.9, 12.1 ppm ° IR (Nujol) 2953, 2924, 2870, 2855, 1659, 1630, 1543, 1454, 1403, 1207, 1196 , 698 cm-1. Elemental analysis found: C, 80.51; H, 7.53. MS (El) i / z 402, 373, 1 20 ,: 91 ° 123) 10-benzyl-3-dicyclopropylformyl 4-Hydroxy-4-hydroxy-5,6,7,8,9,10-hexahydro-cyclooctane [b] nanan-2-- _ isolated 0.0δ5 g of the title product as a white solid. The physical properties are as follows: MP 94-9 7 10. XH NMR (CDCU) δ 7.49, 7.29-7.14, 3.29- 3.21 &gt; 2.89-2.75, 2.22-2. 13,1. 84-1.81, 1.77- 1.55, 1.43 1.31, 1.00-0.86, 0 .53-0. 43 ppm ° 13C HMR (CDCla) δ 194. 4, 164.0, 160. 9, 140. 2, 128.9, 128.3, 125. 9, 111 .9, 105. 0, 40. 9, 39.2 t 37. 3, 35.2, 30.2, 27.1, 25. 6, 23 • 0,12 .4, 12. 2, 3. 6, 3.4, 2.5, 2.2 ppm 0 IR (Hujol) 3000 , 2953, 2922, 2855, 1657, 1631, 1543, 1455, 1231, 1212, 1197τ 1175 cm-1. Elemental analysis found: C, 79.21; Η, 7.98. MS (ΕΙ) ιη / ζ 378, 349, 337, 287, 91 ° -15 4-This paper size is applicable to China National Standard (CNS) A4 (21〇 '乂 297mm) I ------- --Installation ------ Order ---- J--line (please read the note on the back ^^ then fill in -Λ page) No. 83100644 Patent Application Chinese Specification Correction Page (August 1985) A7 B7 V. Description of the invention ((θ) Printed high-resolution measured value by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs: 378.2191. 124) 8-cyclopropylmethyl-4-hydroxy-3-U-benzylpropyl) 5,6,7,8-Tetrahydro-chromen-2-one (Formula L-2 * where iU is ethyl, R2 is -CHz-cyclodiyl, η is 2) See L diagram. 0.108 g of the title product of osmium white solid was isolated. The physical properties are as follows: Μρ 68-73 1. NHR (CDC13) 5 7.43, 7.37, 7.28, 5.82, 4.37-4.31, 2.65-2.64, 2.23-2.21, 2.19-2.12, 2.09-1.99, 1.97-1.89, 1.80-1.45, 1.02, 0.77-0.71, 0.53-0.43 , 0.10-0.09 ppiR ° 13C HMR (CDC13) 5 163.7, 161.0, 141.8, 129.2, 128.5, 127.6, 127.1, 108.4, 106.0, 41.2, 37.4, 37.1, 26.8, 23.9, 20.7, 19.1, 12.3, 8.7, 8.6, 5.3, 3.9 ppa ° IR (Hujol) 2953, 2926, 2855, 1661, 1632, 1551, 1458,] 454, 1403, 1215, cm-1. MS (El) m / z 338, 323, 209. 178, 131, 91. Measured value at high resolution: 3381.881. 125) 9-cyclopropylmethyl-3- (cyclopropyl-phenylmethyl) -4-hydroxy-6, 7,8,9-tetrahydro-5-bucycloheptan [1]] pyridine-2 -_ 0.07 7 g of the title product of osmium white solid was isolated. The physical characteristics are as follows: Mp 77-8310 〇 __- 155 -_ This paper size applies to China National Standard (CNS) A4 specification (2 丨 0X297 mm) (Please read the note on the back before filling this page). , 11 印 Printed Chinese Manual of Patent Application No. 83100644 of the Ministry of Economic Affairs, Consumer Cooperatives, Amendment Page (August 1985) A7 B7 V. Description of Invention ((仏) ^ NMR (CDC13) 5 7.52, 7.38, 7.29 , 6.21-6.20, 3.97, 2.94-2.90, 2.60-2.50, 2.44-2.33, 1.83-1.69, 1.64-1.60, 1.37-1.26, 0.80-0.71, 0.65-0.53, 0.52-0.38, 0.32-0.24, 0.13-0.07 ppb »° 13C HMR (CDC13) 5 165.7, 165.3, 164.0, 140.9, 129.2, 127.9, 127.4, 112.4, 105.6, 44.5, 43.7, 35.4, 28.7, 28.6, 26.6, 26.5, 26.3, 20.7, 13.0, 9.2, 4.9 , 4.1, 3.8, 3.7 ppm 0:-. IR (Nujol) 2951, 2923, 2855, 1654, 1628, 1541, 1 2 0 5 cm _ 1. — 'Elemental analysis found: C, 79.04; Η, 7.60. MS (El) m / z 364, 336, 335, 323, 273, 193, 131, 91, 55. 126) 4-hydroxy-10-methyl-3 (1-phenylpropyl) -5,6 , 7,8,9,10-hexahydro-cyclooctane [b] piperan_ Isolated 0.057 g of the title product as a white solid . The physical characteristics are as follows:

Hp 182-186 ¾ ° XH HMR (CDC13) 6 7.44-7.35, 7.30-7.25, 5.89- 5.82, 4.43-4.33, 3.07-3.00, 2.71-2.61, 2.24-2.12, 2.09-1.98, 1.73-1.521, 1.39- 1.15, 1.29, 1.02 ppm 〇13C NMR (CDC13) 5 165.4, 163.8, 162.9, 162.8, 141.7, 141.6, 129.4, 127.6, 127.3, 111.0, 110.9, __.- 156-_ This paper standard applies Chinese national standard ( CNS) A · 4 size (210X 297mm) —--------- Clothing thread N),-(Please read the note on the back first and then fill in 15 pages) Printed by Chinese Bureau of Consumers' Cooperatives No. 83100644 on the Chinese specification of the patent application (August 85) A7 B7 V. Description of the invention (ϊ $) 106.0, 105.9, 41.3, 41.1, 37.9, 33.5, 33.4, 30.2, 30.1 , 26.9, 26.0, 24.0, 23.9, 22.8, 22.7, 16.9, 12.3, 12.2 ppm ° IR (Hujol) 2954, 2924, 2870, 2855, 1669, 1632, 1546, 1535, 1453, 1206, 1178, cm-1. Elemental analysis found: C, 77.10; Η, 8.19. Measured value at high resolution: 326.1873. 127) 3- (Cyclopropylphenylmethyl) -10-_ethyl-4-hydroxy-5,6,7,8,9,10-hexakis-cyclooctyl [1 &gt;] nane-2-_ 0.103 g of the title product was isolated as a white solid. The physical characteristics are as follows:

Hp 94-98¾ 〇αΗ HMR (CDC13) 5 7.52, 7.38, 7.28, 6.22, 4.01, 2.84-2.70, 2.23-2.14, 2.01-1.97, 1.80-1.51, 1.39-1.31, 0.98-0.86, 0.76-0.71, 0.64 -0.57, 0.32-0.27 p P m ° 13C NHR (CDCU) 5 1 65.7, 163.8, 162.3, 141.1, 129.2, 128.0, 127.9, 127.5, 112.5, 112.4, 106,0, 105.8, 43.8, 43.6, 41.0, 40.9 , 35.7, 30.5, 30.4, 27.3, 25.8, 24.4, 23.1, 13.2, 13.1, 12.8, 5.0, 4.7, 3.8ppm〇- IR (Nujol) 2952, 2924, 2855, 1658, 1632, 1545, 1209, 1196, 1180 Cm-1. Elemental analysis found: C, 78.19; H, 8.11. -157-This paper size applies to Chinese National Standard (CNS) A4 specification (210 '乂 297mm) I --------- installation ------ order ---- jr, .-- line I.i (please read the notes on the back of the page before filling out this page) Printed on the Chinese Manual for Patent Application No. 83100644 by the Consumer Standards Cooperative of the Ministry of Economic Affairs (August 85) (丨 β) MS (EI) m / z 352, 324, 323, 311, 261, 131, 91. 128) 3- (Cyclopropyl-phenylmethyl) -4-hydroxy-10-propyl-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one separation 0.093 g of the title product was obtained as a white solid. The physical characteristics are as follows:

Mp 78-841 :. XH NMR (CDC13) 5 7.51, 7.38, 7.29, 6.23, 4.02, 2.97-2.91, 2.76-2.69, 2.18-2J14, 2.02-1.94, 1.78-1.56, 1.36-1.26, 1.22-1.07, 0.95-0.86, 0.77- 0.71, 0.65-0.57, 0.31-0.25 ppB〇13C NMR (CDC13) S 165.7, 163.8, 162.4, 141.1, 129.2, 128.0, 127.9, 127.4, 112.3, 112.2, 106.0, 105.8, 43.8, 43.6, 38.6, 38.5, 35.9 , 33.4, 30.5, 30.4, 27.3, 25.8, 25.7, 23.1, 21.2, 14.1, 13.2, 13.1, 5.1, 4.7, 3.8 ppm. IR (Nujol) 2955, 2926, 2868, 2855, 1658, 1632, 1546, 1454, 1209, 1196, cm-1. MS (El) m / z 366, 338, 325, 275, 131, 91. Measured value at high resolution: 366.2191. 129) 10-butyl-3- (cyclopropyl-phenylmethyl) -4-hydroxy-5,6,7,8, 9, 10-hexahydro-cyclooctyl [b] piperan-2-one 0.178 g of the title product was isolated as a white solid. The physical characteristics are as follows:

Mp 78-82¾ 〇 __- 158 -_ This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) I -------; --------------------- -J- line (please read the precautions on the back before filling this page) No. 83100644 Patent Application Chinese Specification Correction Page (δ5 years δ month) A7 Β7 V. Description of Invention ((7) HMR (CDCU) δ 丨7.52, 7.38, 7.29, 6.22, 4.01, 2.92- 2.89, 2 • 76-2.69, 2.18- 2.17, 1.98-1.96, 1.78 1.59 , 1.56 -1.46, 1.40-1. 26, 1.23-1.09, 0.93-0.86 0. 76-0.72, 0.64-0.57, 0.32-0.27 ppm 〇 13C HMR (CDCU) δ 165 '6, 163.6, 162.4 * 141.0, 129.1, 127.9, 127 • 8, 127.3, 112.1, 105. 9, 43.7, 43.5, 38. 8 &gt; 38.7, 35. 7, 30 .9, 30.4, 30. 3, 30 .2, 27 .2, 25.6 23.0, 22. 6, 14. 0-,-13.1, 13. 0, 4. 9, (Please read the note on the back first Please fill in this page again.) _ 4.6, 3.7 ppm0 IR (Nujol) 2953, 2922, 2868, 2856, 1657, 1632, 1545, 1402, 1209, 1195 cm -1. Measured value of elemental analysis: C, 78.78; H, 8.68. MS (El) m / z 380, 352, 339, 289, 131, 91 ° High resolution radon measurement: 380.2343. 130) 3- (cyclopropyl-phenylmethyl) -4-hydroxy-10- (tetrahydro-piran-2-ylmethyl) -5,6 , 7,8,9,10-hexahydro-cyclooctyl [b] piperan-2-fluorene isolated 0.41 g of the title product of hydrazone white solid. The physical properties are as follows:

Mp 88-93 T: 〇XW HMR (CDC13) 5 7.50, 7.3, 7.28, 6.19, 4.04- 3.94, 3.42-3.34, 3.21-3.12, 2.70-2.68, 2.26-2.20, 1.80-1.69, 1.61 -1.43, 1.34 -W20, 0.90-0.83, 0.74-0.73, 0.62-0.56, 0.39-0.25 ppm〇13C NHR (CDCI3) 5 165.7, 165.6, 163.9, 162.6, -159-This paper size applies to China National Standard (CNS) Α4 specifications ( 210X297 mm)

1. Printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, printed by the Consumer Standards of the Central Standards Bureau of the Ministry of Economic Affairs, printed No. 83100644, the Chinese specification of the patent application (August 1985) A7 B7 5. Description of the invention (I end 162 5, 141. '1, 129, .3, 129 .2, 128.1, 128 • 0 127. 4, 111 .7, Ill. 6, 106, .0, 105 .9, 74.9, 68.5 * 43 .8, 43.7, 37.7, 34.9, 34., 0, 2.3, 30.4, 27. 3, 27.2, 26.2, 25. 7, 23.6, 23., 0, 13.3, 13.1, 5. 1, 4 .8, 3 · ppm 〇IR (Nujol) 2930, 2854, 1658, 1631, 1546, 1461, 1452, 1403, 1208, 1202, 1181, 1092 cm-1. Measured value of elemental analysis · C, 76.52 .8.27. MS (El) m / z 422, 394, 337, 331, 131, 91. Measured value at high resolution: 422.2465. &Lt; 131) 3- (cyclopropyl · phenylphenyl) -4 -Hydroxy-10 -isobutyl-5,6,7,8,9,10-hexahydro-cyclooctyl [b] piperan-2- _. 0. 073 g of the title product of a white solid was isolated. The physical characteristics are as follows:

Mp 86-9210 〇αΗ NMR (CDC \ 3) δ; 7.51, 7.37, 7., 29, 6.20, 4.01 * 3.03-2.98, 2.74-2.67, 2.21 -2 .18,, 1.99- 1.92, 1. 79 1.. 65, 1.61 -1 .57, 1.34-1. 22, 1. 19-0 .96, 0. 92-0. 87 0 · 75- 0.73, 0 .63-0.58, 0. 29 -0 .28 PP IB 0 13C HMR (CDC U) δ 165.5, 163.6, 162.3, 162.2 3 141.0,, 129.2, 129 • 1 s 128 .1 9 -128. 127 .4, 112. 0, 105.9,, 105.7,, 43.7, 43.5 »40 ^ 2, 40 .1, 36. 3, 36 .0 35 .9, 30.5 9 30.4, 27 .3, 26 • 1, 26.0, 25 .6, 23.2 f 23 .1, 22.4 9 22.3, 13 • 1, 5. 〇, 4. 6, 3.7 ppm 〇-160-This paper size applies to China National Standard (CNS) A4 Specification (210X 297mm) I -------- Installation ------ Order ---- J 丨 line (Please read the precautions on the back before filling this page ) Printing of the Chinese Specification for Patent Application No. 83 100644 by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (August 1985) A7 __B7_ V. Description of Invention (丨 1) IR (Hujol) 2956, 2922, 2868, 2854 , 1658, 1633, 1545, 1465, 1454, 1402, 1209, 1196, Ϊ178 cm-1. Elemental analysis: g, C, 78.7 fe; H, 8.67. MS (El) m / z 380, 352, 339, 289, 131. High resolution measured value: 380.2342. 132; 3- (cyclopropyl) -phenylmethyl) -4-hydroxy-10- (3-methylbutyl) -5,6,7,8,9,10-hexahydro-cyclohex [1 )] Piran-2-hydrazone isolated 0.23 5 g of the title product as a white solid. The physical characteristics are as follows:

Mp 83-881: °… HMR (CDCU) δ 7. 50, 7. 37, 7. 27, 6. 21, 4. 00, 2. 86 -2. 80, 2.75-2 .72, 2. 21- 2.15, 1 • 98-1 '89, 1.77 1.47 * 1.37 -1.26, 1.21 -1. 11, 0. 91- 0 .86, 0. 77-0 .72 0.64 -0 .60, 0.29-0. 28 ppm o 13 C NHR (CDC13) δ 165.7, 165.6, 163.8 * 162. 5, 162. 4, 141 .1, 129 • 3, 129.2, 128.0 9 127. 9, 127 .5, 127. 4, 112.2, 106.0, 105.8, 43.8, 43.7, 39.4, 39.3 9 37.4, 35.9, 35. 8, 30. 5, 30. 4, 29. 2, 29. 1, 28.2 t 28, 1, 27.4, 25. 8, 23. 2, 22. 7, 22.6.2, 13. 3, 13.2 &gt; 5.1, 4.7, 3 .8 p pm ci IR (Nujol) 2954, 2923, 28 6-8, 2854, 1658, 1632, 1546, 1456, 1209, 1195 cm-V0 Measured value of elemental analysis: C, 79.04; Η, 8.75. MS (El) m / z 394, 366, 353, 303, 223, 172, 131, _- 161-This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) ------- -I--install ------ order ---- line (please read the notes on the back ^ and then fill in 1 page) The Chinese Consumer's Manual for Patent Application No. 83100644 printed by the Central Consumers Bureau of the Ministry of Economic Affairs Revised page (δ, 1985) A7 B7 V. Description of the invention ((α) 91 ° High resolution measured value: 394. 2510. 133) 3- (cyclopropyl-phenylmethyl) -4-hydroxy-10- (Tetrahydrofuran-3-ylmethyl) -5,6,7,8,9,10-hexahydro-cyclooctyl [b] piperan-2-one isolated Q. 087 g of the title product as a white solid. The physical characteristics are as follows:

Mp 80-84t: ° &quot; H KMR (CDCU) δ 7.53-7.49, ^ -7; 41-7.36, 7.31, 6.29, 4.06-3.97, 3.92-3.83, 3.79-3.70, 3.40-3.30, 2.99-2.89, 2.79-2.73, 2.22-1.98, 1.80-1.50, 1.40- 1.22, 1.21-1.08, 0.77-0. 71, 0.64-0.56, 0. 32-0.26 PP m ° 13C NHR (CDCla) δ 165.5, 163.7, 161.3, 140.9, 129.3, 128.1, 127.9, 127.5, 112.7, 112.6, 106.3, 73.4, 73.0, 67.9, 43.8, 43.6, 37.9, 37.8, 36.0, 34.5, 34.4, 32.8, 32. 3, 30.5, 30.4, 27.4, 25. 6, 23.3, 13.2, 13.1, 5.1, 4 .7, 3.9, 3.8 ppm ° IR (Nujol) 2953, 2923, 2868, 2855, 1701, 1661, 1 635, 1550, 1452, 1 209, 11 9 8 cm-1. MS (El) m / z 408, 380, 337, 317, 131, 91 〇 Measured value at high resolution: 408.2293. Example 134 3- (Cyclopropyl-phenylmethyl J-4-hydroxy-10- (1-hydroxypropyl) -5,6,7,8,9,10 -Hexahydro-cyclocyclo [b ] Piran-2-_ (Formula L-2, where 1U is cyclopropyl,! ^ 2 is-(^ ((^)--162-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297) (Li) ------------------- 1T ------... (Please read the note on the back # ^ &lt; A6 B6 V. Description of the invention (161) CH2CH3, η is 4) See figure L. A 50-liter three-necked round-bottomed flask with a nitrogen inlet and a 10-milliliter force-equipped addition funnel was charged with diisopropylamine (0.27 Ml) and 2 ml of tetrahydrofuran, and an addition funnel was filled with a solution of the title product of Example 107 (0.249 g) in 4 ml of tetrahydrofuran. The flask was placed in an ice bath, and n-butyllithium (1.15 ml) was added dropwise for 2 minutes. After stirring for 20 minutes at 0 °, the reaction was cooled to -40 t: dry ice / propane bath, and the title product solution of Example 107 was added dropwise for 5 minutes. The addition funnel was wetted with another 1 ml of tetrahydrofuran * And the fresh orange reaction mixture was stirred at -50t: to -30t: for 20 minutes. M was added dropwise for 1 minute. Propionaldehyde (0.17 liters) · and the reaction mixture was stirred for an additional hour when warmed to 50t. The pale yellow solution JfeUO ml 10% hydrochloric acid was stopped, and the children's sodium chloride was added. The reaction mixture was divided into two 30 ml two atmospheres Extracted from methane, dried on magnesium sulfate, filtered and concentrated to produce 0.376 g of clear solids. Up to 25 g of silica gel column chromatography can produce 0.047 g of the title product as a white solid. The physical properties are as follows:

Mp 115-118t. αΗ HHR (CDCla) ^ 7.53-7.49, 7.41-7.36, 7.31, printed by the Shellfish Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before digging into this page). Install J. 6.29, 4.06-3.97 , 3.92-3.83, 3.79-3.70, 3.40-3.30, 2.99-2.89, 2.79-2.73, 2.22-1.98, 1.80-1.50, 1.40-1.22, 1.21-1.08, 0.77-0.71, 0.64-0.56, 0.32-0.26 ppb 0 __ 13C NMR (CDCla) δ 165.1, 163.6, 161.2, 140.7, 129.2, 127.9, 127.8, 1274, 112.5, 106.2, 106.0, -163- This paper uses national standard (CNS) A4 specifications (210X) 297mm ί Printed Chinese Manual for Patent Application No. 83100644 of the Ministry of Economic Affairs's Consumer Cooperatives (Chinese version) (August 1985) A7 ____ B7 V. Description of the invention (f 72.7, 44. 4, 44 .3, 43 , 8, 43.6, 30.6, 30.2, 30.1, 28.6, 27. 5, 27 .1, 25.3, 23.3, 13.1, 13.1, 13.0, 9.9, 5.0, 4 .6, 3.8 ppm 0 MS (EI) m / z 382 , 354, 324, 131, 91 ° measured at high resolution: 382.2137. Example 135 9-but-3-enyl-3- (cyclopropyl-phenylmethyl) -4-hydroxy-6,7, 8,9-tetrahydro-5 [1-treheptan [1)] piperan-2-one (Formula 1-2 * where Ri is cyclopropyl, yes, CH2) 2-CH = CH2, η is 3) See figure L. In a 50 ml round-bottomed flask with a nitrogen inlet and a pressure equilibration funnel of 10 milli ^^, add diisopropylamine (0.36 ml) and 2 ml of tetrahydrofuran * and a solution of the title product of Example 112 (0.242 g) in 4 ml of tetrahydrofuran in an addition funnel. The flask was cooled to -78 t :, and n-butyl hydrazone (U.6 ml) was added dropwise for 2 minutes. . After 5 minutes of searching at -781C, the reaction mixture was stirred at 01C for 20 minutes, and then cooled to -4o. The title compound solution of Example 112 was added dropwise at K for 7 minutes, and the golden solution was stirred at -40T to -201 for 20 minutes. Diiodobutane (0.10 ml) was added dropwise for 1 minute. Once the reaction mixture was warmed to 01: 1, it was stirred for another 2 hours. The pale yellow solution was stopped with 10 ml of 10% hydrochloric acid and a small amount of sodium chloride was added. The reaction mixture was extracted with two 30 ml portions of dichloromethane, dried over magnesium sulfate, filtered, and concentrated to give a golden solid. Chromatography on a 25-g silica column * yielded 0.037 g of the title product as a white solid. The physical characteristics are as follows:

Mp 59-651C 〇 __- 164 -___ This paper is again applicable to the Chinese National Standard (CNS) Α4 size (210 × 297 mm) (锖 Please read the note on the back first ¥ ^ 戽 fill ^ this purchase] 'Central binding department Printed by Chinese Bureau of Standards Consumer Cooperatives No. 83100644 on the Chinese specification of the patent application (August 85) A7 B7 V. Description of the invention (Kp XH HMR (CDC13) 5 7.52, 7.38, 7.30, 6.22, 5.86-5.75, 5.00 , 3.97, 2.83-2.78, 2.56-2.38, 2.20-1.94, 1.88-1.48, 1.47-1.26, 0.77-0.71, 0.65-0.57, 0.32-0.26 ppm® 13C HHR (CDC13) 5 165.5, 165.2, 163.9, 140.9, 137.9, 129.2, 127.9, 127.4, 115.0, 112.5, 105.8, 105.7, 43.7, 43.1, 31.6, 29.5, 28.4, 28.3, 26.5, 26.3, 26.2, 20.7, 20.6, 13.0 ^ 4.9, 3.9, 3.8 ppm. MS (El ) m / z 364, 336, 335, 323, 273, 193, 191, 91, 55 〇-High resolution found: 364.2049. Spring example 136 3-U-benzyl-2-phenyl-ethyl)- 4-hydroxy-5,6,7,8, 9,10-hexahydro-cyclooctyl [b] piperan-2-one (formula J-3, wherein Ri is benzyl, fluorene 2 is benzyl, η is 4) See Figure J. The title can be made by a method similar to that described in Example 107 and Preparation of Compound 48 Compound. 0.042 g of product was isolated as a white solid.

Mp 194- 196 ¾ ° NHR (CDC13) 5 7.45, 7.36, 7.26, 7.18, 6.08, 4.45, 2.77-2.58, 2.47-2.40, 1.74, 1.54 ~ 1.42 pp® ° ES (El) 388, 297, 284, 195 , 194, 91 b / z. Predicted value at high resolution: 388.2038. -Preparation of 45 cyclopropyl- (3-nitrophenyl) methyl

A 250 ml three-necked flask with a thermometer and an addition funnel * was filled with fuming nitric acid (90% * 130 ml) and cooled to -10Ί0. Via liquid adding funnel K _- 165 -_ This paper size is applicable to China National Standard (CNS) A4 (210 '乂 297mm) --------- Gutter (please read the note on the back first) ^ ¾Refill this page) The Chinese Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed the revised Chinese specification of Patent Application No. 83100644 (August 1985) A7 ____ B7 V. Description of the invention Phenyl ketone (21 ml). The reaction temperature was maintained between 茌 -7 and -131: in the addition of ketone. After stirring for another 10 minutes at -IOC, the reaction mixture was poured into 1 liter of crushed ice, 700 ml K Extracted with acetone, washed with two K 5% sodium hydroxide solutions and one brine, dried over magnesium sulfate and concentrated to give 28.14 g of a yellow oil. Recrystallization from 50 ml of methanol yielded 14.62 g of the title product White crystal. The physical properties are as follows: HMR (CDC13) 5 8.86, 8.4-3-, 8.34, 7.70, 2.72, 1.33, 1.17ppra. IR (Nujol) 2954, 2925, 16δΥ, 1614, 1529, 1442, 1386, 1352, 1225, 1082, 1047, 852, 720, 689 cm-1. Elemental analysis found: C, 62.89; Η, 4.73; Ν, 7.32. MS (El) 191 , 1 50, 104, 69 m / z ° Preparation of 46 Cyclopropyl- (3-limylbenzyl) methanone in a Bal hydrogenation tube * Add Pd / C (0.030 g), Cyclopropyl- (3- Nitrophenyl) methanone (Preparation 45) (0. 250 g) and 10 ml of methanol. The tube was shaken overnight at 40 psi hydrogen and room temperature. The reaction mixture was filtered through a plug and concentrated to give 0.207 g of the title product. It can be used without purification. Physical properties are as follows:-HMR (CDC13) § 7.40, 7.2, 7, 7.22, 6.87, 3.87, 2.62, 1.20, 1.02 ppm. Preparation of 47 cyclopropyl- (3-aminobenzyl ester) Phenyl) methanol (Formula J-2, where ______- 1 PI R -___ This paper size applies to China National Standard (CNS) M specifications (210X297 mm) I—n I n II i II order—line. .:} (Please read the note on the back first # fill the goben to buy)

Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs of the People's Republic of China, I No. 831 00644 Patent Application Chestnut Chinese Manual Revised Page (August 85) A7 B7 V. Description of Invention

Ri is cyclopropyl and R2 is meta- (NHC〇2-benzyl) phenyl) see J figure. A solution of 46 cyclopropyl- (3-aminobenzyl) methanol (0.427 g) and diisopropylethylamine (0.55 ml) in 10 ml of dichloromethane was cooled to 0D and benzyl chloroformate was added dropwise. Ester (0.42 ml). The reaction mixture was stirred at the bottom for 15 minutes, and then warmed to room temperature for 2 hours. The reaction mixture was washed with dilute hydrochloric acid, and the aqueous layer was extracted with 2 parts of dichloromethane '. The combined organic layer was dried over magnesium sulfate and concentrated to obtain 0.861 g of cyclopropyl- (3-aminobenzylphenyl) methanone as a brown solid, which was used without further purification. Cyclopropyl- (3-aminobenzyl phenyl ketone (0.861 g) was dissolved in 10 ml of tetrahydrofuran, and 10 ml of formic acid and sodium borohydride (0.601 g) were added. The reaction mixture was stirred overnight at room temperature. Then, it was partitioned into dichloromethane and cold dilute hydrochloric acid. The aqueous layer was extracted with two portions of dichloromethane. The mixed organic layer was dried over magnesium sulfate. It was subjected to silica gel column chromatography (K 40% ethyl acetate). The alkane dissolves) to produce 0.68 δ g of the title product as a pale yellow solid. The physical properties are as follows:

Mp 91-92¾ 〇NHR (CDC13) 5 7.41, 7.39-7.31, 7.26, 7.08, 7.05, 5.16, 3,91, 2.48, 1.16-1.12, 0.59-0.31 ppb0 IR (Nujol) 3414, 3262, 295-5, 2924, 2870, 2855, 1694, 1599, 1559, 1449, 1287 ^ 1262, 1250, 1235, 1054, 1035, 789, 769, 748, 697 cm_110 Elemental analysis found: C, 72.57; H, 6 · 51; N, 4.61. -167 -______ This paper size applies Chinese National Standard (CNS) A4 (210X297 mm) (Please read the notes on the back & fill in this page first) • Binding Printed by the Employees' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Revised Page of Chinese Specification for Patent Application No. 83100644 (August 85 &gt; A7 B7 V. Description of Invention ((Recognition) MS (El) m / z 297, 269, 253, 225, 91 〇 Preparation 48 1,3- Diphenyl-2-propanol (Formula J-2, where Ri is benzyl * R2 is benzyl) see J diagram ° Three necks of a liquid addition funnel in a 50 ml, equipped with nitrogen inlet and 60 ml pressure equilibrium A round bottom flask * was charged with lithium aluminum hydride (2.27 g), and 100 ml of acetic acid, and cooled to Ot :. The addition funnel was filled with l3-diphenylpropyl copper (10.23 g) in 20 ml of ether The solution was added dropwise to the reaction mixture for 30 minutes. After stirring at room temperature for 18.5 hours, the reaction mixture was cooled to 0¾ * and 3 ml of water and 10 ml of 1H hydrogen were added dropwise. Sodium oxide. The reaction mixture was stirred for an additional 30 minutes at room temperature. The solution was triturated with magnesium sulfate and concentrated. * 10.57 g of the title product was produced as a colorless oil. It can be used without re-oxidation. The physical properties are as follows: NMR (CDC13) 5 7.34-7.30, 7.25-7.22, 4.07, 2.91-2.73 ppn »° Example 137 Ethylene sulfonic acid (3- (1- (4- Hydroxy-2-oxy-2H-chromen-3-yl) -propyl) -phenyl) -amidamine; or [2-[[[[3-: l- (4-hydroxy-2-oxy- 2H-1-benzopiperan-3-yl) propyl] phenyl] amino] sulfofluorenyl] vinyl] -p-14.7 mg 3- [1- (3-aminophenyl) propyl]- Add 4-ml-coumarin to 1 ml of dichloromethane and 8.1 microliters of pyridine. Add 5.71 microliters of ethylsulfonium at room temperature and avoid ice vapor. Allow the reaction mixture to stir at room temperature for 3 minutes. Hours. Add 5 ml of dichloromethane and wash with 5 ml of solution K. The organic solution is dried, dried and dried over anhydrous sodium sulfate. -1 «« This paper size applies to Chinese National Standard (CMS) A4 specifications (210 × 297 mm) ---------- install -------- order ---- 1, I line, -I /, j: one (please read the precautions on the back &amp; (Refill this page ¾) Printed on the Chinese Manual for Patent Application No. 83 100644 by the Consumer Standards Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (August 85) A7 B7 Explanation (丨 q becomes the crude title product. Chromatography on 15 g of silica gel, using 5% methanol / aqueous imitation, and collecting the substance with Rf = 0.3 can produce 6.3 mg of the title product. 0 Physical properties are as follows: HRMS detection Value: 386. 1059. Example 138 Ethanesulfonic acid (3- (1- (4-hydroxy-2-oxy-2H-chromene-3-yl) propyl) -phenyl) -fluorenamine; or [2-[[[ 3- [1- (4-hydroxy-2-oxybenzopiperazin-3-yl) propyl] phenyl] amino] sulfonyl] ethyl]-14.75 mg 3- [1- (3- Aminophenylpropylpropyl] -4-hydroxy-coumarin was dissolved in 1 ml of dichloromethane * and 8.1 microliters of pyridine was added. To this solution, 5.14 microliters of ethyl sulfonate was added at room temperature and in the absence of water. Brew chlorine. The reaction was allowed to stir at room temperature for 18 hours. 5 ml of dichloromethane was added to the reaction mixture. The resulting mixture K1 ml was washed twice with water, and the dichloromethane solution was separated, dried over anhydrous sodium sulfate, It was evaporated to dryness to produce 28 mg of the crude title product. Chromatography on 15 g of silica gel with K 5% methanol / chloroform as the solvent yielded 6.8 mg of the pure title product. The physical properties are as follows: = 0.14; 5 % Methanol / Chloroform. Spring Example 139 2- (1,3-dioxy-1,3-dihydroisoindobor-2-yl) ethanesulfonic acid (3- (1- (4-hydroxy-2 --Oxy-2H-chromen-3-yl) · propyl) phenyl) fluorenamine; or [U [[3-[(1- (4-hydroxy-2-oxybenzopiperan- 3-yl) propyl] phenyl] amine ] Sulfofluorenyl] ethyl] -phthaloimine]--16 9-This paper size applies to Chinese national standard (CMS> A4 specification (210 X297 mm) I ---------- Select this ------ 1T ---- y # — '1 ”(Please read the note on the back 3, and then fill out 1 page) Printed by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 83100644 patent Correction page of the manual (August 85) A7 B7 V. Description of the invention 10.1 mg of the title product. The physical properties are as follows:

Rr = 0.5 in 5% methanol / chloroform. HRMS detection value: 533.1384. Example 140 2- (H-Third. Butoxycarbonyl-amino) -ethanesulfonic acid (3-U- (4-hydroxy-2-oxy-2H-chromen-3-yl) -propyl) -Phenyl) -amidamine; or carbamic acid di,-[2-[[[[[[ To 31 mg of the title product of Example 139, 6 ml of 95% ethanol was added to 31 mg of phenyl] phenyl] amino] sulfofluorenyl] ethyl]-, 1,1-dimethylethyl ester. A solution of 3.2 ml of 100 µl / 100 ml of hydrazone in 95% ethanol (3.2 µl of hydrazine hydrate) was added at room temperature. After stirring for 48 hours, an additional 3 ml of hydrazine hydrate solution was added, and the reaction was allowed to stir at room temperature for a further 96 hours. The reaction mixture was evaporated to dryness under vacuum and triturated twice with 5 ml of ethyl acetate. The resulting residue was chromatographed on 15 g of silica gel. M 25% methanol / chloroform was used as the eluent to produce 11 mg of unsecured aminosulfonamide. The physical properties are as follows: = 0.3 in 25% methanol / chloroform. MS detection value: 403. 1319. To 8 mg of the amine compound was added 2 ml of a 1: 1 di-Bf alkane dihydrate aqueous solution * and when the solution was complete, 20 mg of BOG-OH + 2 drops of triethylamine were added. After stirring for 15 minutes, the reaction mixture was evaporated to dryness. The residue was dissolved in ethyl acetate and chromatographed on 10 g of silica gel using 35% ethyl acetate / hexane as the dissociation-170-This paper applies Chinese national standards (CNS) A4 size (210X297 mm) ---------- Meal ------ ir ----) 1 ^ (Please read the notes on the back and fill in this page again) A6 B6 printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (1). All unreacted BOC-ON was collected and the eluent was changed to 25% methanol / atom. The material with RF = 0.75 (25% formazan / aqueous paraffin) was collected, evaporated to dryness, dissolved in chloroform (with trace amounts of methanol), and processed and evaporated to dryness to produce 10 mg of the pure title product. The physical characteristics are as follows: MS detection value: 503.1858. Examples 141-160 141) 4-Hydroxy-7- (2-morpholin-4-yl-ethoxy) -3- (1-phenylpropyl) -chromen-2-one Physical properties are as follows: HRMS : 409.1889 ° 142) 4-hydroxy-3- (1-phenyl-cyclopropyl) -chromene-2-moe Physical properties are as follows: HRMS: 278.0942 ° 143) N- (2-hydroxy-indan-I-yl ) -3- (1- (4-hydroxy-2-oxy-2H-chroman-3-yl) -propyl) -benzylamine The physical properties are as follows: HRMS: 455.741 0 ′. 144) 3- (1 -Benzylpropyl) -4-hydroxy-chromen-2-one physical properties are as follows: MW found: 294; found: C, 77.40LH, 6.29. 145) The physical properties of 3- (1-benzyl-3-phenylpropyl) -4-hydroxy-chromen-2-one are as follows: -171- This paper size is in accordance with China National Standard (CNS) A4 specification (210X297 (Mm) (Please read the notes on the back before filling in this page). Binding · Binding · -Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 _B6_ V. Invention Description U7〇) HRMS: 370.1569 ° 146) 3- ( The physical properties of 1-benzyl-2-phenylethyl) -4-hydroxy-chromene-2-fluorene are as follows: HRMS: 356.1412 ° 147) 3- (1-benzylbutyl) -4-hydroxy-chromene -2- 特性 Physical properties are as follows: MW found: 308; 'Found: C, 78.00; H, 6.51. 148) Benzimidazol-2-ylmethyl) -3- (1- (4-hydroxy-2-oxy-2H-chromen-3-yl) -propyl benzamidine Physical properties are as follows: HRSM: 454.1758 〇149) 3- (1- (4-hydroxy-2-oxy-2H-chromen-3-yl) propyl) -N- (2-methyl-1- (pyridin-2-ylmethyl) The physical properties of carbamoyl) butyl) -benzylamine are as follows: HRMS: 528.2506 ° 150) Acetic acid 4-(1- (4-hydroxy-2-oxy-2H-chromen-3-yl) -methyl. · Ethyl) -phenyl ester physical properties are as follows: HRMS: 339.1232 〇151) 4-hydroxy-7- (2- (2-methoxy-ethoxy) -ethoxy) -3- (1-benzene The basic physical properties are as follows: (Please read the precautions on the back before filling out this page) 'Packing-172- This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) ) A6 B6 5. Description of the invention (171) HRMS: 398.1729 ° 152) 3- (2,2-dimethyl-1-phenylpropyl) -4-hydroxy-chromen-2-one Physical properties are as follows: HRHS : 308.1417 〇153) 4-hydroxy-6 ', 3 * -dimethyl-3', 4 * -dihydro-2 * [{-[3 ', 4'] dicarene-2 -fluorene154) 4 -Ethyl-7- (2- (2-methoxy-ethoxy)>-ethoxy) ethoxy ) -3- (1-phenyl-propyl) -chromene-2-fluorene physical properties are as follows: HRMS: 442.1991 ° 155) 3-U-ethyl-3-phenylpropyl) -4-hydroxy-color The physical characteristics of enenone are as follows: MW found: 308; found: C, 77. 86; H, 6.74. 156) 3-U-ethyl-4-phenylbutyl) -4-hydroxy-chromene-2-fluorene The physical properties are as follows: MW found: 322. 157) 2-((4-hydroxy- &lt; 2-oxy: 2 氧基-, chromen-3-yl) phenyl-methyl) -malonate The physical properties are as follows: Found: C, 64.8 ; Η, 4.87; 0.00. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page)-Pack 158) ] Dichromene-2- 醑 159) 3-U-benzyl-1,2,3,4-tetrahydro-quinolin-4-yl) -4-hydroxy-trypene-2-one-173-benzyl Paper size applies to the ten national standards (CNS) A4 specifications (210X297 mm) A6

5. Description of the invention (172) The physical characteristics printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs are as follows: S: 383.1510 ° 160) 4-hydroxy-3- (3-hydroxy-phenylphenyl) chromene-2- 烯The physical properties are as follows: HRMS: 296.1041 ° Example 161 3- (Cyclopropylbenzylmethyl) -5,6,7,8,9,10-hexaaza-4-hydroxy-10- (2-hydroxy-1- Methylethyl) -211-cyclooctyl 1 ^] lanan-2-face (formula L-2, where η is 4, Ri is cyclopropyl 'R2 is -CH (CH3) (CH2〇H) &gt; See circle L. Following the general procedure of Example 121 without any change in identity, but replacing the bromomethylcyclopropane with M propylene oxide, 0.017 g of the title compound was obtained as a white solid. The physical properties are as follows: HRMS: 382.2139 MS (El) m / z 382, 354, 337, 291, 166, 131, 91. Measured value at high resolution: 382.2144. Example 162 3- (Fluoropropylphenylmethyl) -5,6,7,8,9, 10-hexahydro-4-hydroxy-iq- (2- via fluorenylcyclooctyl [b] pyran-2-fluorene (·. · '· Formula L-2, where η is 4 and IU is cyclopropyl, R2 is -CH2-CH (CH3) (0H)) See L. Using the above steps, 0.010 g of the title compound was obtained as a white solid. The physical properties are as follows:- HRMS: 382.2137 MS (El) m / z 382, 354, 337, 291, 166, 131, 91, -174- This paper size adopts China National Standard (CNS) A4 specification (210X297) ¢ Please read first Note on the back, please fill in this page again.) Installation • Lamps • Printed by the Central Bureau of Standards, Ministry of Economic Affairs, Printed by Aigong Consumer Cooperative A6 B6 5. Description of the invention () 45 〇 Measured value at high resolution: 382.2144. Example 163 3- (Cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4, hydroxy-10- (oxiranylmethyl) -2H-cyclooctyl [b] pyran The 2--2-ketone follows the general procedure of Example 121, but there is no discernible change, and the K-methane methoxypropane ring is substituted for bromomethylcyclopropane to obtain 0.031 g of the title compound as a white solid. The physical properties are as follows: Low-resolution mass spectrum : 380, 352, 337, 322, 289, 171, 131, 91 〇MP 67-71t: (decomposition). MS (El) m / z 380, 352, 337, 322, 289. 171, 131, 91 〇 Ao 49 Cyclopropyl- (3-nitrophenyl) formamidine (Formula M-2) See figure M. For a 1 liter sheathed three-necked round-bottomed flask with a stirrer and an addition funnel, under nitrogen Add 580 liters of fuming nitric acid and cool to -40t :. Slowly add 1.5% propyl phenyl ketone (formula M-1) (100 g) and keep the temperature at -351C. Stir for 3 hours and follow the reaction by TLC. Pour the mixture into 3 kg of ice / water. K3x 500 ml of acetamidine acetate extraction. The mixed organic calendar was washed with 2 x 1.5 liters of a saturated aqueous sodium bicarbonate solution, dried over magnesium sulfate, filtered, and concentrated to yield 138 g. The residue was dissolved in 270 ml of methanol, cooled to -20¾ for 18 hours, filtered, and the filter cake was washed with cold methanol. The product was dried under reduced pressure for 72 hours to obtain 63.86 g. GC Analysis-175- This paper size is in accordance with Chinese National Standard (CNS) A4 specification (210X297 mm). Please read the instructions on the back of the paper (on this page again)-Packing .. Order. Central Ministry of Economic Affairs Printed by the Consumer Bureau of Standards Bureau A6 __B6__ 5. Description of the invention (174) (15 a. 08-1.1 '. = 100 &lt; 〇, 10 it / min, 1 ^-6.0 points) shows the substance &gt; 98% purity. The physical properties of the title compound are shown above Preparation 45. Preparation 50 Cyclopropyl- (3-aminophenyl) methanone (Formula M-3) See M picture Pd / C (8.7 g) was charged into a Barr bottle. Into the flask were added cyclopropyl (3-nitrophenyl) methanone (86.7 g) and formazan (156 liters) for preparation 49, and the solution was heated and dissolved in an ice bath and cooled to 9¾. Hydrogenated for 50 minutes, the temperature was maintained at 35 ° F, and the reaction was followed by MTLC. The reaction mixture was filtered through flocs and concentrated to 70 g under reduced pressure. The physical properties are as follows: aH NMR (CDC13) 5 7.99, 7.47-7.19, 6.84, 3.84, 2.60, 1.23-1.15, 1.03-0.96 ppm ° 13C NMR (CDC13) 5 200.9, 146.8, 139.1, 129.4, 119.3, 118.4, 113.9, 17.2, 11.6 ppm ° Preparation of 51 Cyclopropyl- (3-aminophenyl ester phenyl) methanone (Formula M-4) See Figure M. At the bottom of the 3-liter mechanical mixer and liquid addition funnel In a flask, add (under nitrogen) Preparation 50 of cyclopropyl- (3-aminophenyl) methanone (7 0.0 g), diisopropyl Z1 amine (DIPEA, 90.2 ml) and dichloromethane (CH2C12) ( 113 liters). The reaction mixture was cooled to 0 ° :. Dichloromethane (67.5 ml) was diluted with dichloromethane (186¾ liters) and added to the substrate solution, which was maintained at 0-5C for 1 hour. Can form a thick precipitate. It was heated for 1.5 hours by the M stirring method, and the reaction was followed by M TLC. The reaction mixture was poured into 600 ml of IN HC1 / 600 g of ice / 4.2 liters of dichloromethane and stirred to dissolve. The layers were separated, and the organics were dried over magnesium sulfate, dried over, and reduced to dryness. Slurry solid -176-^ Paper size it uses China National Standard (CNi) A4 ^ (210x2 ^ 7mm) &lt; Please read the precautions on the back before filling this page)

J Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 B6 V. Description of the invention (Π5) The body particles were dried in 3 ml / gram of the courtyard and dried under vacuum to 25 grams. The physical properties are as follows: NMR (CDCla) 5 8.01, 7.76-7.69, 7.43-7.33, 7.18, 5.21, 2.64, 1.25-1.20, 1.03-0.97 ppb ° 13C NMR (CDCU) 5 200.6, 153.4, 138.7, 13B.5, 135.9, 129.3, 128.6, 128.4, 123.1, 122.8, 118.1, 67.2, 17.3, 12.0 ppm. Preparation 52 Cyclopropyl- (3-aminobenzylbenzyl) formase (Formula M-5) was found in a 2-liter three-necked draw-bottom flask with an overhead stirrer, and the cyclopropyl-51 was added under nitrogen. (3-Aminophenylbenzyl) formamidine (25 g) 'tetrahydrofuran (THFM 450 ml) and ethanol (90 ml). The reaction mixture was cooled to 0-5t :, and the sodium borohydride (12.4 g> Nine Canadians) was divided into three equal portions at 30 minutes. Warm it to 23t :, and stir for another 20 hours. Track the reaction by TLC. The reaction mixture was cooled to 0-5 ° C, and 90 ml of 1N hydrochloric acid was added to stop it slowly. The temperature was kept at 10 t: M. Pour methylene chloride (600 ml) and 1N hydrochloric acid (400 ml) under stirring. Layer, and washed the organic drawer (1 liter) with a saturated sodium chloride solution. It was dried over sulfuric acid, filtered and concentrated to 23.7 g. The physical properties are as follows: TH NMR (CDC13) 5 7.41-7.35, 7.33. 7.17, 7.10, 5.17, 3.93, 2.36, 1.16-1.12, 0.60-0.32 ppb ° 1SC HMR (CDC13) 5 153v5, 145.0, 137.9, 136.1, 129.0, 128.6, 128.3, 121.2, 117.9, 116.5, 67.9, 67.0, 19.1, 3.6 , 2.8 ppb0 -177- This paper size is applicable to the national standard (CMS) A4 specifications (210X297 public love 7 (please read the precautions on the back before filling in this page). Binding. Consumption by employees of the Central Standards Bureau of the Ministry of Economic Affairs Cooperative printed No. 83100644 of the Chinese Application for Patent Application Amendment Page U5 Aug. 5) A7 B7 V. Description of Invention (| · / [) Example 164 3-U3-Aminephenyl) cyclopropylmethyl] -5,6,7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piper-2.-one (Formula M-7) See M. In a 100 ml three-necked round bottom flask with a reflux condenser and nitrogen inlet, add 10% Pd / C (1.0 g) to the product of formula M-6 (Example 119) (1.95 G) In a mixture of cyclohexane (50 ml), the mixture was refluxed for 4 hours. The mixture was then passed through a plug, washed with K dichloromethane (CH2CU), and K was concentrated to give 1.25 g of the title product as a white solid dimer. The physical properties are as follows: Μ · P. 75-79 °…. IR (Hujol) 2995, .2951, 2921, 286S, 1660, 1619, 1605, 1590, 1551, 1491, 1460, 1447, 1428, 1404, 1247, 1226 , 1202, 1191, 1172, 1127 cm-1. MS (El) m / z 339, 310, 213, 187, 159 ° Examples 165-169 Using similar procedures to the above, the following other compounds of the invention can be prepared. Example 165 Urethane, [3-[[3- [Cyclopropyl (4-hydroxy-2-oxy-2H-1-benzopiperan-3-yl) methyl] phenyl] amino] -3-ketopropyl]-, 1,: 1- The physical properties of dimethyl ethyl ester are as follows:-NMR δ 0.04, 0.18, 0.38r, 1.23, 2.32, 3.22, 6.7-7.3, 7.82, 7.96 ° Example 166 aminocarboxylic acid * [3- [cyclopropyl ( 4-Hydroxy-7-methoxy-2- -178-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) -------, &lt; ------------- --Order ---- J-line (please read the notes on the back%. Buy it again) Printed Chinese Manual of Patent Application No. 83100644 by the Consumer Standards Cooperative of the Ministry of Economic Affairs (August 85) A7 B7 V. Description of the invention ((rsoxy-2H-1-benzopiperan-3-yl) methyl] • phenyl]-, phenylmethyl ester The physical properties are as follows: H + 471.1672 ° Example 167 Amine group Formic acid * [3-[[3--[Cyclopropyl (4-hydroxy-7-methoxy-2-oxybenzopiperan-3-yl) methyl] phenyl] amino] -3-_ Propyl ]-, 1 / 1-Dimethyl ethyl ester physical properties are as follows: aH HMR δ 0.05, 0.23, 0.40, 1.29, 2.35, 3.37, 3.62, 6.39, 6.85, 7.06, 7.25V7.7〇 Example 168 Fragrant B · , 4-Cycloyl-3- (〇 {-(3-((3-((3-() ^-'s-1--1-yl)-: 1-ketopropyl) amino) phenyl) cyclopropylmethyl The physical properties are as follows: NMR δ 0.30, 0.46, 0.7, 1.9, 2.73, 3.6, 4.45, 6.39, 7.0-7. 6, 7.9. Example 169 Coumarin, 4-hydroxy-3-U-phenylpropyl ) -7-Propoxy has the following physical properties: M. 338.1524. Examples 1 7 0-1 9 5 Using the procedure described in Example 121 (see Figure L), the compounds of the present invention can be prepared:-Example 170 3- (Cyclopropyl Phenylphenylmethyl) ^ 5,6,7,8,9,10 -hexahydro- 4-hydroxy-10-U tetrahydro-2-furanyl) methyl] -2H-cyclooctyl [b] Nanan- 2-_ -179-This paper size is in accordance with Chinese National Standard (.CNS) A4 (210X297mm) --------- binding ^ order ~ line (please read the notes on the back before filling it ^ (This page) Patent Application No. 83100644 Revised Chinese Manual U5 δ Month) A7 .. _ Β7 V. Description of Invention ((^) Printed by the Consumers' Cooperative of the China Standards Bureau of the Ministry of Economic Affairs 0.039 g of the title compound was isolated as a white solid. This compound was isolated from the same reaction mixture as in Example 171 and was a more polar stereoisomer. &lt; · The physical properties are as follows: MS (El) η / ζ 408, 380, 337, 191, 131, 91, 71. High resolution measured value: 408.2300. Example 171 3- (Cyclopropylphenylmethyl) -5,6,7,8,9,10-Hexahydro- 4-hydroxy-10-[(tetrahydro_2_pyridyl &gt; methyl) -2Η-cyclooctane [b] piperan-2-_ Isolated 0.017g of the standard hydrazone product as a white solid. This compound was isolated from the same reaction mixture as in Example 170, and was a relatively non-polar stereoisomer. The physical properties are as follows : MS (EΠ m / z 408, 380, 337, 191, 131, 91, 71. Measured value at high resolution: 408.2300. Example 172 3- (cyclopropylphenylmethyl.)-5,6,7, 8, 9, 10-hexahydro-4-hydroxy-10- [2- (2-methoxyethoxy) ethyl] -2H-cyclooctane [b] piperan-2-one Isolated 0.032 g Compound, white solid. Physical properties are as follows: MP 129-133 = 0.-XW HMR (CDC13) 5 7.51, 7.3 ^, 7.30, 6.26, 6.24, 4.04, 3.98, 3.61-3.39, 3.38, 3.36, 3.29-3.21 , 2.76-2.67, 2.30-2.17, 1.86-1.73, 1.66-1.60, 1.19- -180-(Please read the note on the back ##-^^ Fill on this page first) Binding line This paper size applies Chinese national standards (CNS) A4 Specification (210X297 mm) Patent Application No. 83100644 Revised Chinese Manual (δ5 Aug) A7 B7 V. Invention Theory (Gf) 1.07, 0.79-0.72, 0.66-0.56, 0.32-0.26 ppm. 13C HMR (CDC13) 6 165.5, 163.7, 161.6, 161.5, 140.9, 129.1, 128.1, 127.9, 127.8, 127.4, 112.6, 112.5, 106.0, 105.8, 71.9, 69.8, 69.1, 58.9, 43.7, 43.5, 35.5, 35.1, 35.0, 31.0, 30.4, 30.3, 27.1, 25.6, 22.9, 13.1, 13.0, 5.0, 4.6, 3.7 ppiDOIR (Hujol) 2996, 2952 , 2923, 2868, 2854, 2856, 1653, 1613, 1537, 1453, 1404 ;,-1 198, 1 177, 1 155, 1 136, 1 1 16, 1085 cm-1. MS (El) m / z 426 , 398, 350, 337, 335, 322, 179, 131, 91, 59, 45 ° At high resolution: 426.2406. Example 173 3- (Cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-10- (hydroxymethyl) -2H-cyclooctyl [b] piran -2- 嗣 isolated 0.076 g of the title compound as a white solid. The physical properties are as follows: MP 110-113Ό (decomposed). HMR (CDC13) 5 7.50, 7.38, 7.29, 4.78-4.10, printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 3.99, 3.93, 3.77-3.72, 3.22-3.17, 2.78-2.70, 2.28 -2.17, 1.77-1.65, 1.62 -1.48, 1.43-1.26, 0.77-0.71, 0.6 3-0. 5 5, 0.3 2-0 '2 7 p i &gt; in 〇13C NHR (CDCl3) 8 165.4, 1jS3.9, 160.4, 140.9, 140.8, 113.0 , 112.9, 106.5, 106.3, 63.1, 43.9, 43.7, 42.2, 42.1, 31.6, 31.5, 29.9, 29.8, 26.8, -181 — This paper is again applicable to China National Standard (CNS) A4 specifications (210X297 mm) Article 83100644 Revised page of the Chinese manual for the patent application No. (85 months in 1985) A7 B7 V. Description of the invention ((25.5, 22.6, 13.1, 13.0, 5.0, 4.7, 3.9, 3.8 ppm. IR (Nujol) 3266, 3077, 3061, 3025, 2998, 2953, 2924, 2855, 1667, 1636, 1553, 1453, 1404, 1378, 1210, 1199, 1184, 1137, 1045, 697 cm-1. MS (El) m / z 354, 326, 313, 295, 263, 131, 91 ° Measured value at high resolution: 354.1831. Example 174 3- (Cyclopropylphenylmethyl) -5,6,7,8, 9, 10-hexahydro-4-hydroxy-10-U-ketopropyl Cyclooctyl [b] piperan-2-one isolated the title compound of 0.013 g of a hydrazone white solid. The physical properties are as follows:… MP 71-76T (decomposed). MS (El) m / z 380, 352, 324, 296, 295, 289, 131, 91, 57 〇Measured value at high resolution: 380. 1987. Example 175 3- (cyclopropylphenylmethyl) -5,6,7,8,9,10 -hexahydro-4 -Hydroxy-10-U-hydroxy-bumethylethyl) -2H-cyclooctane [b] piperan-2-one. 0.067 g of the title compound was obtained as a white solid. The physical properties are as follows: MP 223-225¾ ° IR (Nujol ) 3216, 3082, 3053, 3022, 2952, 2925, 2854, 1663, 1655, 1630, 1559 „4δ1, 1456, 1374, 1267, 1250, 1220, 1165, 1134, 695 cm-1. Elemental analysis found: C, 74.92; Η, 8.05. 182 This paper size applies Chinese National Standard (CNS) A4 specification (210 × 297 mm) Please read first page Gutter No. 83100644 Patent Application Chinese Specification Correction Page (August 85 &gt; A7 B7____ V. Invention Explanation (θΙ) MS (ΕΪ) m / z 382, 367, 324, 296, 295, 131, 91, 59 ° Measured value at high resolution: 382. 21 44. Example 176 10- (cyclopropylhydroxymethyl) -3- (cyclopropylphenylmethyl)-5,6,7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctane [b] piperan-2-one was isolated in an amount of 0.059 g. The title compound is a white solid. Physical properties are as follows: ^ MP 107-115Ό (decomposed). 13C NMR (CDC13) δ 165.5, 165.1, 161.3, 160.7, 141.0, 140. 9, 129.3, 128.1, 128.0, 127.6 , 127.5, 113.4, 112. 5, 106. 1, 76. 1, 75 .6, 46. 4, 46 • 3, 45.6, 44.0, 43.8, 43.7, 31.6, 30.9, 30.8, 30.4, 30.3, 27.6, 27.5 , 27.2, 25.5, 23.5, 23.2, 22.7, 17.1, 16.9, 16.8, 14.1, 13.3, 13.2, 5.1, 4.9, 4.8, 4.4, 4 .0, 3.9, 3.8, 3.6, 3.5, 2.4, 1.8 ppm 0 IR (N uj ο 1) 3252, 3078, 3065, 3024, 3000, 2953, 2925, 2856, 1666, 16 37, 1555, 1454, 1402, 1 378, 1265, 1242, 1210, 1197, 1137, 1034, 1018, 697 cm_ 1 〇 MS (El) ro / z 394, 324, 296,-295, 131 〇 Ministry of Economic Affairs Printed on the High Resolution Spring of the Consumer Standards Cooperative of the Central Bureau of Standards: 394.2144. "Example 177 3- (Cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro- 4-hydroxy -10- (Methoxymethyl) -2H-cyclooctane [b] piperan-2-_ -183-This paper size applies to China National Standard (CNS) A4 (210X297 mm) Employees of the Central Standards Bureau of the Ministry of Economic Affairs Consumption Cooperative printed No. 83100644 of the Chinese Patent Application Specification Revised Page (August 1985) A7 B7 V. Description of the invention 0.085 g of the title compound, a white solid, was isolated. The physical properties are as follows: MP 70-78 C (decomposition). XH NMR (CDC13) 5 7.50, 7.37, 7.30, 6.25, 4.02, 3.95, 3.92-3.88, 3.52-3.47, 3.39, 3.38, 3.34-3.23, 2.76-2.69, 2.22-2.18, 1.75-1.72, 1.64-1.46, 1.42-1.31, 0.77-0.71, 0.63-0.56, 0.31-0.27 pp®〇13C NMR (CDCla) 5 163.7, 160,0, 140.9, 140.8, 129.1, 128.0, 127. 9,127 .8, 127.4, 112.5, 106.4, 72.8, 59.0, 43.89, 43.6, 39. 9, 39.8, 32.0, 31.9, 30.1, 30.0, 26.9, 25.3, 22.8, 13.1, 13.0, 5.0, 4.6, 3.9, 3.7 ppmc &gt; IR (Hujol) 3076, 2922, 2855, 1661, 1548, 1 460, 1431, 1405, 1209, 1134, 708, 696 cm-1 O MS (El) m / z 368, 340, 327, 295, 271, 131, 91, 45 ° at high resolution Found: 368. 1982. Example 178 3- (Cyclopropylphenylmethyl) -5,6,7,8,9,10-Hexahydro- 4-hydroxy-10- (2-methoxyethyl) -2H-cyclooctyl [ b] Piran-2-m isolated 0.039 g of the title compound as a white solid. The physical properties are as follows: r MP 78-δΟ ”. ΑΗ HMR (CDC13) 8 7.50, 7.38, 7.29, 6.23, 4.03, -184-This paper size applies to China National Standard (CNS) A4 (210X 297 mm)- ---------------- Private clothes ------ IT ---- i ';). One by one (Please read the note on the back | ^ before filling this page) ___ I:, _1! ------ -.— '-&quot; Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 83100644 Patent Application (Chinese Version Correction Sheet U5 August 2015) A7 B7 V. Description of the Invention ((D) 3.98, 3.47-3.44, 3.32-3.31, 3.21-3.16, 2.96-2.90, 2.72-2.60, 2.46-2.42, 2.26-2.18, 1.78-1.53, 1.37-1.30, 1.23-1.08, 0.79-0.72, 0.66-0.54, 0.32-0.27 ppm0 IR (Hujol) 3074, 2924, 2855, 1659, 1547, 1495, 1455, 1403, 1377, 1209, 1135, 1123, 1086, 707, δ96 cm. 1 〇MS (El) m / z 382, 337, 43 °? Measured value at high resolution: 382.2 2136. Example 179 3- (CyclopropylphenylmethylΓ-5,6,7,8,9,10-hexahydro-4- Hydroxy-10-[(tetrahydro-2H-piperan-3-yl) methyl] -2H-cyclooctane [b] piperan-2-one isolated 0.047 g of the title compound as a white solid. The physical properties are as follows: M P 89-95 T: ° aH NMR (CDC13) 5 7.54-7.49, 7.41-7.35, 7. 3 1-7.27, 6.27-6.21, 4.05-3.96, 3.88-3.84, 3.38-3.30, 3.13-2.94, 2.79- 2.69, 2.16-2.08, 1.95-1.51, 1.43-1.14, 0.78-0.69, 0.65-0.58, 0.33-0.25 ppm. 13C HMR (CDC13) 5 165.4, 163.6, 163.5, 161.4, 161.3, 140.9, 140.8, 140.7,- 1 29.2, 129.1, 128.1, 128.0, 127.9, 127.8, 127.4, ^ 12.4, 112.2, 106.2, 73.3, 73.1, 68.4, 68.3, 43.7, 43.5, 36.1, 36.0, 35.6, 35.5, 34.3, 34.1, 34.0, 33.8, 33.7, 30.4, ___- 185 -_ This paper size applies to China National Standard (CNS) A4 (210X 297 cm) I -------- ^ 衣 ------ ΐτ ---- l — A \ ιι... .--- (Please read the note on the back ^ t before filling in this ￥ 0 August) A7 B7 V. Description of the invention (r) 30.3, 30.2, 30.0, 37.2, 25.7, 25.5, 23.2, 13.1, 13.0, 5.0, 4.6, 3.8, 3.7 ppm ° IR (Nujol) 3173, 3025, 2924 , 2853, 1660, 1550, 1495, 452, 1402, 1383, 1209, 1134, 1094, 1031, 1017, 967, 707, 69 6 cm _1. MS (El) m / z 422, 394, 337, 331, 131, 97, 91 〇 Measured value at high resolution: 422.2456. Example 180 3- (Cyclopropylphenylmethyl) "-. 6,7,8,9-tetrahydro-4-hydroxy-9- [2- (2-methoxyethoxy) ethyl] -cyclo Heptane [b] piperan-2 (5H) -one isolated 0.025 g of the title compound as a white solid. The physical properties are as follows: NMR (CDC13) 5 7.51, 7.32, 7.30, 6.24, 3.98, 3.58-3.55, 3.39, 3.02-2.94, 2.50-2.44, 2.29-2.19, 1.88- 1.48, 1.37-1.25, 0.78-0.71, 0.68 -0.58, 0.32-0.25 ppn Example 181 3- (Cyclopropylbenzylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- [2- [2- (2-methyl Oxyethoxy) ethoxy] ethyl] -cyclohepta [b] pyran-2 (5H) _one isolated 0.048 g of the title compound as a colorless gum. The physical properties are as follows: HMR (CDC13) 5 7.52, 7.3, 8, 7.3 1, 6.25, 3.96, 3.68-3.53, 3.38, 3.01-2.95, 2.51-2.45, 2.28-2.17, 1.88- 1.50, 1.42-1.26, 0.79- 0.71, 0.68-0.57, _; _- 186-_ This paper size is applicable to Chinese national standard 〇 (〇 ^) 8 4 specifications (210 乂 297 mm) I ---- ^ ------ pack- ----— Order ----- Λ ~ line (please read the precautions on the reverse side and fill it in | page). No. 83100644 Patent Application Chinese Specification Revision Page U5 Years September) A7 _______B7 V. Invention Explanation (丨 buckle) 0.32-0.25ppm ° Example 182 3- (Cyclopropylphenylmethyl) -6,7,89_tetrahydro-4_hydroxy-9- (phenylmethyl) -cycloheptane [b ] Piran_2 (5H) -one fractionated 0.047 g of the title compound as a white solid. The physical properties are as follows: MP 178-1 82 ¾ ° 2H NMR (CDCU) 5 7.52, 7.42-7.19, 6.24, 3.97, 3.25-3.1 9, 3.12-3.10, 2.83, 51-2.48, 1.89-1.86 * 1.73-1.43, 1.35 -1.30, 0.88-0.78, 0.76-0.74, 0.66-0'59, 0 · 30 · 0 · 28 ppm〇13C NMR (CDCU) δ 165.1, 164.5, 163.8, 140.9, 139.4, 129.2, 129.0, 128.6, 128.5, 128.3, 128.0, 127.9, 127.4, 126.2, 112.8, 105.9, 105.8, 45.5, 43.8, 43.7, 36.3, 29.6, 27.6, 27.4, 27.1, 26.8, 26.0, 20.8, 20.7, 13.0, 5.0, 4.9, 3.8 ppm . IR (Hujol) 3072, 2924, 2855, 1665, 1641, 1542, 1508, 1496, 1451, 1425, 1203, 1187, 1166, 1134, 750, 702 cm-1. MS (El) ra / z 400, 372, 309, 131, 91 ° printed at the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs, measured at high resolution: 400.2037. Example 183 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (2-methylpropyl) cyclopenta [b] piperan-2 ( 5))-0.141 g of the title compound was isolated as a white solid. The physical characteristics are as follows; ____- 187 -____ This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 × 297 mm) The Chinese Specification for Patent Application No. 83100644 printed by the Central Standards Bureau of the Ministry of Economic Affairs (Chinese version) Month) A7 B7 V. Description of the Invention (ί 绛) MP 164-167 ^ 0. &quot; H HMR (CDC 1 3) δ 7. 52, 7.38, 7.30, 6.19, 2.98, 2.90-2.78, 2.60-2.50, 2.47-2.38, 1.84-1.46, 1.38-1.26, 0.97, 0.90, 0.80-0.71, 0.65-0.58, 0.32-0.26 PP m ° 13C HMR (CDC13) 6 166.3, 165.3, 164.1, 141.1, 129.3, 128.0, 127.5, 112.4, 105.8, 43.9, 41.5, 39.3, 28.8, 28.7, 26.7, 26.5 ^,- 26.4, 25.5, 23.2, 23.2, 22.1,20.9, 20 · 8, 13.1,5.0, 4.0 ppm. IR (Mujol) 2955, 2854, 1654, 1541, 1495, 1404, 1378, 1205, 1140, 961, 705 cm-1. MS (El) m / z 366, 338, 325, 310, 275, 249, 195, 172,131,91 ° High resolution measured value: 366.2191. Example 184 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (3-methylbutyl) cyclohepta [b] piperan-2 (5H )-嗣 Isolated 0.056 g of the title compound * as a white solid. The physical properties are as follows: MP 67-77 t: 〇αΗ HMR (CDC'13) 5 7.52, 7.38, 7.30, 6.24, 6.21, 3.98, 2.79-2.73, 2.52-2. 43, -1.86-1 .50, 1. 34-1.18, 0.90, 0.77-0.74, 0.65-0. 60, 31-0 .27 ppm 〇 1 3C HMR (CDCU) δ 166.1, 165.3, 164.1, 141.1, 129.3, 128.0, 127 • 5, 112. 3, 105.7, 44.2, 43.9, -18 8-This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) -------- ^-installation ------ order-- --7 ^ 1 line —. One by one. (Please read the note on the back # ^ before filling out this note) The Employees Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs printed the revised Chinese manual for the patent application No. 83100644 (δ5 years 8 Month &gt; A7 ___ B7 V. Description of the invention (丨? 36.9, 36.8, 28.6, 28.4, 28.2, 28.1, 26.6, 26.4, 26.3, 22.8, 22.5, 20.8, 13.1, 5.1, 5.0, 4.0 ppm〇IR (Nujol ) 3060, 2925, 2855, 1655, 1542, 1495, 1462, 1405, 1383, 1231, 1204, 1171, 1140, 1017 · 705 cm-i. MS (ΕΙ &gt; ib / z 380, 352, 289, 131. High resolution found: 280.2340. Example 185 3- (Cyclopropylphenylmethyl)-. 9, ethyl-6,7,8,9-tetrahydro -4-Hydroxy-cycloheptan [b] piperan: 2 (5H) -one was isolated as the standard compound of 0.089 g of a white solid. The physical properties are as follows: MP 63-71¾ NMR (CDCU) δ 7.52, 7.38, 7.31, 6.24 -6.21, 3.96, 2.79-2.67, 2.57-2. 35, 1.97-1.44, 1.38-1.23 0.97, 0.80-0.71, 0.65-0. 58, 0.32-0.26 ppm 〇 13C NMR (CDC 1 3) δ 165.9, 165.4, 164.1, 141.1, 129.3, 128.0, 127.5, 112.4, 105.7, 45. 6, 43.9, 28.4, 28.3, 26.7, 26.5, 26.4, 23.6, 20 .8, 13. 1, 12.3, 5.1, 4.0 ppm 〇IR (Nujol) 3060, 2924, 2856, 1654, 1540, 1495, 1460, 1404, 1378, 1226, 1205-, 1 170, 1 130, 705 cm_ 1 〇e- MS (El) m / z 338, 310, 309, 297, 247, 221, 131, 91 〇 ------ m, the two paper sizes are applicable to Chinese national standards (CNS ) A4 size (210X297mm) I binding line J, one-T- (please read the note on the back &quot; \ then fill in this page) No. 83100644 Patent Application Chinese Manual Correction Page (August 85) A7 B7 V. Description of the invention (Measured value at high resolution: 338.1 884. Example 186 3- (Cyclopropylphenylmethyl) -9- [2- (1,3-dioxocene-2-yl) ethyl] -6,7,8,9-tetrahydro-4- Hydroxy-cyclohepta [b] piperan-2 (5H) -one isolated 0.042 g of the title compound as a white solid. The physical properties are as follows: MP 68-7 6 ^. XH NMR (CDCU) 5 7.52, 7. 3θ, 7.30, 6.23-6.19, 4.89, 4.00-3.91, 3.87-3.75, 2.82-2.78, 2.58-2.39, 2.06-1.97, 1.82-1.51, 1.35-1.22, 0.77- 0.71, 0.64- (Please read the note on the back 4 before filling out this page)-Packing. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 0.61, 0.31-0, 2 4 ppm ° 13C NMR (CDC13) δ 165.3, 165.2, 164.0, 141.1, 129.3, 128.0, 127.5, 112.6, 105.9, 104.3, 64.9, 43.9, 43.7, 31.9, 28.8, 28.7, 2 6 .6, 2 6.4, 26. 3, 24.8, 20.8, 13.1, 5.1, 4.0 ppm 0 IR (H uj ο 1) 3060, 2922, 2855, 1656, 1544, 1495, 1454, 1 405, 1378, 1206, 1139, 1033, 962, 945, 776, 7 0 5 cm-1 O MS (El) hi / z 410, 382, 322, 294, 131, 99, 91,73 Measured value at high resolution: 410.2089 °-Example 187 3- (Cyclopropylphenylmethyl) ^ 6,7,8 , 9-tetrahydro-4-hydroxy-9-[(tetrahydro-2H-piperan-3-yl) methyl] -cycloheptane [b] piperan-2 (5H) -fluorene

、 1T line-190-This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 83 100644 Patent Application Chinese Version Correction Sheet (August U5 Aug. 5) A7 B7 V. Description of the invention (ίί |) 0.080 g of the title compound was isolated as a white solid. The physical properties are as follows: MP 82-90C ° αΗ NMR (CDC Is) δ 7 .52, 7. 38, 7 .30, 6. 24 -6. 20, 3. 97, 3. 90-5 ί. 8 6 &gt; 3.42-3. 34, 3.15 -3. 04, 2. 89-2.70, 2. 56- 2.36, 1.96 -1.41, 1. 39-1.13, 0.8 8 ~ 0.71, 0.65- 0. 59, 0. 32-0 丨. 26 ppa ° 13C HMR (CDC1 3) δ 165. 3, 1 2 65; 1, 164.0 0, 141.0, 129.3, 128.0 丨, 127 • 6, 112 .7, 106.0, 73. 6, 73. 2, 68.6, 68 • 5, 43. 9, 40 • 6, 40. 5V 3 3 .6, 33 .3, 33 .2, 30 .4, 29. 3, 29. 2, 28 '0, 27. 9, 27 .1, 26 .9, 26 .8, 26 .3, 25 .8, 25. 6, 20 • 9, 14. 1, 13 .1, 5. 1, 4.0 ρρη 0 IR (Hujol) 3060, 2924, 2854, 1658, 1546, 1495, 1453, 1404, 1378, 1204, 1139, 1094, 1032, 1017, 7 0 5 cm-1. MS (El) m / z 408, 380, 323, 131, 97, 85. In high-resolution estimation: 408.2300. Found: 408.2304. Example 188 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9-propyl-cycloheptan [b] piperan-2 (5H) -one was isolated 0.089 g of the standard-title compound as a white solid. The physical properties are as follows: r MP 60-65t :. HMR (CDCU) 5 7.52, 7.37, 7.30, 6.22, 6.19, -191-This paper size applies to China National Standard (CNS) A4 (2 丨 0'〆297mm) — gutter., I./J! (Please read the notice on the back before filling in this page.) Employee Consumer Cooperation of the Central Bureau of Standards of the Ministry of Economic Affairs Du printed No. 83100644 Patent Application Chinese Manual Correction Page (August 1985) A7 B7__

V. Description of the invention (IS 3.97, 2.81-2.72, 2.57-2.50, 2.46-2.36, 1.89-1.39, 1.35-1.29, 0.96-0.92, 0.78-0.71, 0.63-0.58, 0.31-0.26 ppm 0 13C HHR (CDCU ) S 166.0, 165.9, 165.3, 164.0, 141.0, 129.2, 127.9, 127.4, 112.3, 105.6, 43.8, 43.6, 32.5, 29.6, 28.6, 28.5, 26.5, 26.3, 20.8, 20.7, 14.0, 13.0, 4.9, 3.9 P p ffl 0 IR (Hujol) 3025, 2927, 2856 ”1654, 1542, 1495, 1456, 1403, 1378, 1204, 1131, 1017, 705 cm-1. MS (ED in / z 352, 324, 1 31 Γ 91 〇Measured at high resolution spring: 352.02042. Spring Example 189 3- (cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9-[(tetrahydro-2-furan Methyl) -cycloheptan [b] piperan-2 (5H) -one isolated 0.068 g of the title compound as a white solid. 丨 Physical properties are as follows: MP 74-88t: (decomposition) aH HHR (CDC13) 5 7.52-7.50, 7.39-7.35, 7.30- 7.28, 6.21, 3.98-3.88, 3.87-3.81, 3.74-3.69, 3.03 -3.01, 2.54-2.43, 2.20-2.00, 1.94-1.82, 1.75-1.43, 1.33-1.32 , 0.78-0.71, -0.64-0.58, 0.31-0.28 ppm «Wide IR (Hujol) 3060, 2921, 2856, 1656, 1543, 1495, 1458, 1404, 1378, 1206 1139, 1074, 1051, 1017, -19 2-* This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) --------- t .------, order ---- •. · .1 .- (Please read the note on the back first ^, and then fill out this page) No. 83100644 Patent Application Chinese Specification Correction Page (August 1985) A7 B7 V. Description of Invention ( No) 7 0 6 cm-1. Elemental analysis found: C, 75.73; H, 7.86. MS (El) Bi / z 394, 366, 323, 131, 91 ° High resolution found: 394.21 44. Example 190 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9-[(tetrahydro-2H-piperan-2-yl) methyl] -cyclo Hept [b] piperan-2 (5H) -m isolated 0.082 g of the title compound as a white solid. The physical characteristics are as follows: (Please read the note on the back before filling out this page). Equipment-Printed by the Consumers Cooperative of the Central Standards Bureau, Ministry of Economic Affairs, MP 76-86 10 (decomposed). aH HHR (CDCla) δ 7.52, 7.39, 7.30, 6.27-6.18, 3.99-3.93 ,: 3.42-3.24, 3.18-3.03, 2.50 -2 .46, 2.12 1 · 96, 1.81-: 1.71, 1. 66 -1. 47, 1. 33-1. 29, 0. 79- 0.70 0 · 63-0 .58, &lt; D. 32- 0. 24 ppm O 13C HMR (CDC1 3) δ 165. 9, 165.3, 164.1 t 141 .1, 141.0, 129 .: 3, 129.2, 128 .2, 128. 〇, 127. 5, 112.5 , 105.7, 75.3, 75 .2, 68 .5, 68 .4, 43.9, 43.8, 39.9, 39 • 8, 39.7, 38. 4, 38. 3, 37. 0, 32 .4, 32.3 , 30 .9, 30 • 6, 29.0, 28. 9, 28. 0, 27. 6, 27 .4, 26. 3, 26 • 1, 23 .6, 23.5, 21. 1, 21. 0, 20 . 9, 13 • 2, 1 3. 1, 5. 0, 43.0, 4.0 ,; 3.9 ppm O _ IR (Hujol) 3060, 2997, 294 ^, 2923, 2854, 1656, 1629, 1 544, 1461 , 1454, 1 404, 1378, 1 233, 1202, 1176, 1139, 1089, 1050, 705 cm-1.

, 1T line -193-This paper size is applicable to Chinese National Standard (CNS) A4 specification (210 × 297 mm) Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 831 00644 Patent Application Exhausted Chinese Manual Revised Page (δ August 5 ) A7 B7 V. Description of the invention ((, 彳 MS (El) n / z 408, 380, 323, 131. Measured value at high resolution: 408.2292. Example 191 3- (Cyclopropylbenzylmethyl)- 0.07 g of 6,7,8,9-tetrahydro-4-hydroxy-9-[(tetrahydro-3-furyl) methyl] -cycloheptan [b] piperan-2 (5H) -one isolated The title compound is a solid. The physical properties are as follows: MP 80-84 = 0 (decomposition)... HHR (CDCU) δ 7.53, 7.41: 7.36, 7.30, 3.96, 3.92- 3.83, 3.79-3. 72, 3.38, 3.32, 2.82-2. 77, 2.55 -2.46, 2.44-2.38, 2.29-2.23, 2.06 -1.98, 1. 81- 1.46, 1.36-1.26, 0 .78-0.71, 0.65- 0.58, 0. 31-0.26 PP m ° 13C HMR (CDC 1 3) 8 165.1, 1 64.0, 140.9, 129.3, 128.0, 127.6, 112. 8, 106.0, 73.4, 73.2, 67.9, 43.9, 42.9, 37.4, 37.3, 34.2, 33. 9, 32.8, 32.7 , 32.2, 29.5, 29.4, 29.0, 28.9, 26. 9, 26.7, 26.5, 26.3, 20.8, 13.1, 5.0, 4.0 ppm ° IR (Hujol) 3075, 3060, 2923, 2856, 1700, 1657, 1 545, 1495, 1454, 1403, 1378, 1265, 1205, 1102, 1020, 7 0 5 cm-1.-MS (El) m / z 394, 366, 223 131, 91 ° Measured value at high resolution: 394.2131. Example 192 3- (cyclopropylphenylmethyl) -6,7,8,9 -tetrahydro-4-hydroxy- 19 4-This paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) —--------- ^ Winter Order 'W. Line (Please read the note on the back first ^ &lt; then fill in 1 (This page) Printed by the Consumer Standards Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs, No. 83100644, Chinese Patent Application Specification Correction Page (August 1985) A7 B7 V. Description of Invention ((p) -9- (2-hydroxypropyl) ring Heptane [b] piperan-2 (5H) -_ Isolated 0.151 g of the title compound as a white solid skull. The physical properties are as follows: MP 8b 84υ (decomposed). &quot; H HMR (CDC13) 5 7. 52-7.50, 7.40-7. 35, 7.31- 7.28, 3.95, 3.89, 3.. 16-3.03, 2.51-2.45, 2.09-1.99, 1.83-1.54, 1.29-1.23, '0.77-0.72, 0.62-0.58, 0.32-0.25ppm〇IR (Nujol) 3281, 2995, 2922, 2854, 1663, 1548, 1495, 1456, 1405, 1377, 1208,' 1 130, 1017, 705 cm-1 〇MS (ΕΙ) ιη / ζ 368, 350, 340, 323, 233, 179, 152, 131, 91 〇 High resolution measured value: 368. 1996. Example 193 3-(Cyclopropylphenyl'methyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (methoxymethyl) -cyclohepta [b] piperan-2 ( 5H) -one isolated 0.075 g of the title compound as a white solid. The physical properties are as follows: MP 69-7110 〇aH HRR (CDCla) 5 7.54-7.49, 7.41-7.35, 7.32-7-29, 6.25, 3.95, 3.82-3.76, -3.59, 3.40, 3.10-3.07, 2.63-2.55, 2.40-2.32, «1.93-1.84, 1.73-1.53, 1-47-1.42, 1.37-1.30, 0.77-0.71, 0.66-0.57, .0.31- 0. 2 6 pp ® 〇 _________-195-___ Paper size Applicable to China National Standard (CNS) A4 specification (210X297mm) I--1 n Winter I I 11 Order * —I line ί: First, (Please read the note on the back before filling this page) Central Bureau of Standards, Ministry of Economic Affairs Employee Consumer Cooperative Co., Ltd. printed the revised Chinese specification of Patent Application No. 83100644 (August 85) Α7 ___ Β7 V. Description of Invention 13C HHR (CDC] 3) 5 165.0, 163.7, 162.9, 140.8, 129.1, 128.0, 127.4, 113.4, 106.0, 71.7, 58.8, 43.8, 43.7, 28.3, 28.1, 25.8, 25.9, 25.8, 21.0, 20.9, 13.0, 4.9, 4.0, 3.9 ppm ° IR (Hujol) 3060, 2924, 2855, 1657, 1544, 1495 , 1455, 1406, 1378, 1205, 1 138, 1 125,706 cm-1. Elemental analysis found: C, 74.72; H, 7.68. MS (El) m / z 354, 326, 31 3, 2 281, 263, 131, 91, 45 ° High resolution measured value: 354.1832. ^ Spring Example 194 3- (cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (2-methoxyethyl) -cyclohepta [b] piperan- 2 (5H) -one isolated 0.09 8 g of the title compound as a white solid. The physical properties are as follows: HP 58-60 t: (decomposed). 1W NMR (CDC13) 5 7.51, 7.38, 7.29, 6.26, 3.96, 3.46, 3.33, 2.99-2.96, 2.50-2.45, 2.23-2.17, 1.87 -1.50, 1.34-1.32, 0.77-0.72, 0.64-0.57, 0.31- 0.26 ppm〇13C HHR (CDC13) 5 165.1, 140.9, 129.2, 128.0, 127.9, 127.4, 1 12.7, 105.?. -70.7, 70.6, 58.6, 43.8, 40.4, 30.7, 29.5, 29.4〇27.3, 27.1, 26.1 , 20.9, 20.8, 13.0, 4.9, 3.9 ppm. IR (Hujol) 3076, 3060, 2922, 2856, 1556, 1543, -19 6 ~ This paper size is applicable to China National Standard (CNS) A4 size (2IOX297 mm) 丨 .I ----- 1 Binding · Line ( Please read the note on the back ^^ before filling out this page) Printed Chinese Manual of Patent Application No. 83100644 by the Ministry of Economic Affairs of the Ministry of Economic Affairs Amendment Page (August 1985) A7 _B7 V. Description of the Invention (1495 , U56, 1404, 1378, 1204, 1138, 1119, 1017, 7 0 6 cm-1. Elemental analysis spring measurement: C, 74.77; H, 7.94. (El) m / z 368, 340, 323, 131, 91, 43. Measured value at high resolution: 368.1993. Example 195 9- (cyclopropylhydroxymethyl) -3- (cyclopropylphenylmethyl) 7,8,9-tetrahydro-4-hydroxy-cyclo Hept [1]] piran-2 (5 ^ 1) -one isolated 0.168 g of the title compound of white solid. The physical properties are as follows: MPδδ-Θ0 ,. HMR (CDCU) δ 7.52-7.48, 7.38, 7.30, 6.30, 4.00-3.93, 3.44-3.31, 3.03-29.8, 2.61-2.54, 2.49-2.36, 1.97-1.47, 1.35-1.30, 1.15-1.01, 0.9S- 0.83, 0.76-0.71, 0.63-0.56, 0.43-0.32, 0.31-0.26 ppm. IR (Kujol) 3281, 3077, 2925, 2855, 1662, 1548, 1455, 1404, 1378, 1205, 1139, 1032, 1018, 702 cm-1. MS (El) m / z 380, 310, 131 〇 High resolution found: 380. 1980. Example 196 Urethane, [3-[[3- [cyclopropyl (5,6,7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2-H-cyclooctyl [ b] piperan-3-yl) methyl] phenyl] amino] -3-one diyl]-, 1,1-dimethylethyl ester (formula 2, where R1®2-Ht-B0C -Ethylamine) See Figure 0 -197-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) ------------ Private Clothing ----- 1T ---- _.: (Please read the notes on the back ^ before filling this page) No. 831 00644 Revised Chinese Manual of Patent Application (August 1985) A7 B7 A 25ml nitrogen-containing two necks A round bottom flask was charged with a compound of formula N-1 (prepared in Example 164 (0.050 g)), Nt-BOC- / S-alanine (0.028 g) * triethylamine (0.030 g), and dichloromethane ( 10 ml). At 0 t: bis (2-oxy-3-Dfazolidinyl) phosphine phosphonium chloride (0.0375 g) * was added and the solution was stirred at room temperature for 1 hour. Water (0.8 mL) and 4N hydrochloric acid (3 drops until acidic) were added, and the mixture was extracted with dichloromethane (30 mL). The organic layer was reduced to 0.07 g. Chromatography on 15 g of silica gel yielded 0.055 g of the title compound as a white solid. The physical properties are as follows: MP 197-1 98.5¾ (decomposed). … &Quot; H HMR (C0C13) 6 8.01, 7.60, 7.55, 7.31, 7.20, 3.90, 3.46, 2.63-2.52, 2.47, 1.73, 1.64-1.56, 1.43, 0.77-0.73, 0.63-0.51, 0.29-0.25 ppm. 13C HMR (CDCU, DMSO) δ 169.0, 163.8, 163.3, 159.4, 154.9, 143.5, 137.4, 127.0, 122.0, 118.1, ----------- install-'' i (Please read first Note on the back ^^ Please fill in this page again), ιτ The Indian consumer policy of the Central Government Bureau of the Ministry of Economic Affairs 116.4, 109.5, 105. 4, 77 .6, 44 .0, 39. 0, 35 .8, 29.9, 28.3, 27.8, 27.4, 25.2, 24.6, 21.3, 11.6, 5.6, 2.9 pp in ° IR (Hujol) 3445, 3259, 3100, 3086, 2954, 2922, 2868, 2856, 1714, 1679, 1656, 1641, 1614, 1592, 1561, 1452, 1437, 1398, 1377-, 1 366, 1 342, 1254, 1218, 1198, 1182, 1172, 1 142rv 10 5 4 cm-1. Elemental analysis found: C, 67.72; Tb, 7.54; N, 5.33 ° MS (El) m / z 510, 437, 410, 381,339,310,57. LINE-198-This paper size applies Chinese National Standard (CNS) A4 specification (21〇χ297 mm) No. 83〗 00δ44 Patent Application Chinese Specification Correction Page (August 1985) A7 B7 V. Description of Invention (丨 77 ) Printed by High-resolution Analytical Value: 510. 2731. Example 19 7-2 1 2 Using the procedure of Example 196 above (see Figure N) *, other compounds can be prepared as follows: Example 197 1 Indole-bupropionamine, N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl.] Phenyl]-isolated 0.042 g of the standard compound as a white solid. The physical properties are as follows: MP 199-204t: °… &quot; H HMR (DMS0) 5 10.38, 9.87, 7.52, 7.45, 7.31, 7.17-7.11, 7.00, 6.39, 4.48, 3.10-3.06, 2.80, 2.55-2.80, 1.81 , 1.63, 1.55, 1.43-1.38, 0.68, 0.42-0.38, 0.22-0.18, 0.11-0.07 ppm ° 13C HMR (DMSO) δ 168.7, 163.9, 163.5, 160.3, 144.5, 138.6, 135.6, 128.6, 128.2, 127.9, 122.5, 121.1, 120.5, 119.0, 118.4, 116.7, 110.1, 109.9, 106.0, 100.7, 45.7, 44.6, 37.1, 30.3, 29.2, 28.7, 25.9, 25.4, 21.9, 12.4, 6.6, 3.8 ppm ° IR (Nujol) 3261 , 3104, 2953, 2922, 2868, 2855, 1682, 1660, 1640, 1616, 1594-, 1562, 1464, 1458, 1441, 1402, 1377, 1368, 1261〇1216, 1203, 1184, 744 cm-1. MS (El) m / z 510, 482, 130 〇-199-This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) (Please read the note on the back before filling this page). 燊.- \ β Printed by the Consumer Standards Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, No. 831 00644 of the Chinese Patent Application Manual (August 85) A7 B7 V. Description of the invention (丨 f /) Measured value at high resolution: 510.2516. Example 198 Urethane, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) methyl, phenyl] phenyl] amino] -1- (S) -methyl-2-oxoethyl]-, 1, 1-dimethylethyl ester was isolated in a quantity of 0.28 g and The title compound as a white solid. The physical properties are as follows: MP 134-1391 (decomposed). -. &Quot; H NHR (CDC13) 5 8.55, 7.60, 7.49, 7.30-7.17, 5.04, 4.30, 3.88, 2.61, 2.46, 1.73, 1.66-1.47, 1. 4 5, 1 · 4 2, 0.7 2, 0.6 1-0.5 0, 0.2 δ-0.2 3 ppm ° 13C NMR (CDCU) 5 170.8, 165.6, 164.1, 161.3, 142.2, 129.7, 129.6, 123.8, 123.7, 119.0, 118.7, 110.7, 106.0, 50.7, 43.8, 30.7 , 29.1, 28.8, 28.2, 26.2, 25.8, 25.7, 22.1, 17.2, 12.9, 5.0, 3.8 ppdi〇IR (Hujol) 3299, 2953, 2925, 2855, 1669, 1660, 1612, 1593, 1557, 1489, 1 455 , 1446, 1405, 1393, 1376, 1367, 1249, 1 202, 1170, 10 7 0 cm-1. MS (ED m / z 511, 510, 455, 411, 340. High resolution found: 51 1.2831.-Example 199 Aminocarboxylic acid, [2-[[3- [Lingpropyl (5,6, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino]-: l- [n- (S)-[(4-methylphenyl) sulfo-200-This paper size is applicable to China National Standard (CNS) A4 specification (2I0X297 mm) I -------- installation ------ Order ----- Line ί / Two ...-. (Please read the note on the back before filling out this page) -¾ & 3100644 Patent Application Checking Chinese Revision Book Correction Page (August 1985) A7 B7 V. Description of the invention ((fi) fluorenyl] -1H-imidazol-5-yl] methyl-2-ketoethyl]-, 1, 1-dimethylethyl ester 0.39 g white foam The title compound is a solid. The physical properties are as follows: MP 120-1 24Ϊ: (decomposition) aH HMR (CDC13) 6 9.85, 8.59, 7.88, 7.51, 7.39, 7.28-7.15, 6. 55, 5.92, 4 .79 V 3. 90, 3.43-3 .29, 3.02-2 .89, 2. 59, 2. 49-2. 40, 2, 45, 1.74, 1. 61- 1.36, 1.32, 0 .74, 0 .58-0 .51, ° · 27 ΡΡΙΒ ° 13C KMR (CDCla) δ 165.6, 161.6, 161.3, 146.3, 142.3, 138.1, 13 6 .0, 130 .5, 130 .4, 130.1, 129.6, 127.2, 126 .9, 123 .8, 119 .1, 118 .7, 115.0, 114.9, 110.7, 105 .9, 43. 8, 30. 7, 30.5, 29 .9, 29. 1, 28.9 28.1, 26.2, 25.7, 22.1, 21. 6, 14.1, 13.0, 5.0, 3.8 ppa 〇IR (Nujol) 3297, 2953, 2923, 2868, 2854, 1672, (Please read the note on the back ^ * ^ before filling out this page). Install. Printed by the Consumer Cooperatives of the Central Elevator Bureau of the Ministry of Economic Affairs 1612, 1595, 1558, 1488, 1467, 1456, 1446, 1401, 1378, 1368, 1 342, 1308, 1 278, 1249, 1221, 1191, 1174, 1127, 1 093, 1082, 1049, 1018, 703, 675, 609 cm_ 1 ο MS (El) m / ζ 731, 631, 577 ,-477, 264, 1 10 ° Measured value at high resolution: 731.3137. r Spring case 200 Limb formic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piran-3-yl) A-201-This paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm). Printed Chinese Manual for Patent Application No. 83100644 by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. August 1985) A7 ____ B7 V. Description of the invention (&gt; ^) group] benzyl] amino] -2-oxoethyl]-, 1, dimethyl ethyl ester isolated 0. Π5 grams of mixed The title compound as a white solid. The physical characteristics are as follows: MP 114-124TM decomposition). NHR (CDCla) δ 8.30, 7.55, 7.49, 7.31-7.21, 5.30, 3.90- 3 * 86, 2.60, 2. 46, 1.74, 1.57-1 .48, 1.47, 0.75,, 0.60- 0.51, 〇.28 -ppm Ο 1 3C NMR 1 (CDC 1 3) δ 167.8, 165.7, 164.1, 161.3, 156 • 2, 142. .4, 137.9, 129.6, 'V23 .8, 119.3, 118.7, 110 .7, 106. 45. 4, 43.9, 30 .7, 30 .2, 29. 1, 28.8, 28. 2, 26.2,, 25.7, 22.1, 12.9, 5.0 .0, 3.8 ρ ρ m 0 IR (Hujol) 3299, 2953, 2924, 2855, 1670, 1661, 1612, 1594, 1557, 1516, 1489, 1455, 1 445, 1405, 1394, 1367, 1279, 1267, 1250, 1231, 1 203, 1171 cm_1. MS (El) m / z 497,496,441, 423,397,340,247,146,57. Measured value at high resolution: 497.2635. Example 201 Aminocarboxylic acid * [4-[[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4 * Ethyl-2-oxy-2- 2-ri-cyclooctyl [b] Nan-3-yl) methyl] phenyl] amino] -4-oxofluorenyl]-, 1,2-dimethylethyl ester isolated 0.192 g of the title product as a white solid. -202-This paper adopts China National Standard (CNS) A4 (210X297 mm) I --------- ^ ------, order ----- one one (1— '. (Please read the lack of attention on the back # before filling in this page) No. 83100644 Patent Application Chinese Chestnut Revision Sheet (δδ, 1985) ^ V. Description of Invention (p |) Printed by the Consumers' Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs The physical properties are as follows: MP 188-191 υ (decomposition). MMR (CDC13) 5 8.87, 7.76, 7.62, 7.30, 7.17, 6.41, 4.79, 3.93, 3.24, 2.61, 2.45-2.36, 1.91- 1.82, 1.75-1.71 , 1.66-1.47, 1.45, 0.75, 0.62-0.55, 0.30-0.25 ρρβι ° 13C HMR (CDC13) 5 171.2, 165.7, 164.0, 161.2, 157.1, 142.1, 139.0, 1 29.7, _-123.5, 118.8, 118.6, 110.7 , 106.0, 79.8, 43.7, 39.2, 34.4, 30.7, 29.1, 28.8, 28.2, 27.1, 26.2, 25.7, 22.0, 13.0, 4.9, 3. 8 pp ta ° IR (Hujol) 3357, 3002, 2996, 2954, 2922 , 2855, 1771, 1663, 1653, 1621, 1594, 1562, 1545, 1454, 1443, 1402, 1390, 1386, 1363, 1332, 1219, 1211, 1198, 1183, 1169, 1159, 1123 cm-i. HS ( El) m / z 525, 524, 425, 340, 247, 86, 5 70. Measured value at high resolution: 525.2999. Spring example 202 (S) -pyrrolidinecarboxylic acid, 2-[[[3- [cyclopropyl (5,6,7,8,9,10 -hexahydro) -4 -Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3 -yl) methyl] phenyl] amino] amino]-, ι, ι-dimethylethyl ester isolated 0.317 grams of white solid standard compound. The physical properties are as follows: MP 132-136¾ (decomposed) ◊ -203 This paper size applies to China National Standard (CNS) Α4 specification (210X297 mm) ---------- -1-- (Please read the notes on the back before blowing this page)

, 1T Line No. 831 00644 Patent Application Revised Chinese Specification (August 85) A7 B7 V. Invention Description (& HMR (CDC13) 5 7.68-7.49, 7.29, 7.18, 6.38, 4.45, 3.92, 3.45 -3.38, 2.78, 2.64-2.42, 1.92, 1.75-1.7 1, 1.66-1.55, 1.48, 0.73, 0.63Ό.54, 0.29-0.24 ppm〇13C NMR (CDC13) 5 164.0, 161.2, 129.8, 123.7, 123. 6,123.5,118. 8, 118 .7, 118.6, 118.5, 110.7, 106. 1, 105.9, 80.9, 47.1, 43.7, 43.6, 30.6, 29.1, 28.8, 28.3, 26.2, 24.4, 22.0, -13.0, 12.9, 4.9 , 3.8 PP m ° IR (N uj 〇1) 3286, 2953, 2924, 2868, 2854, 1701, 1667, 1668, 1661, 1593, 1557, 1488, 1 479, 1455, 1445, 1437, 1404, 13 7 8 , 1368, 1247, 1234, 1201, 1163, 11 2 6 cm -1 ° MS (El) m / z 5 3 6, 463, 436, 339, 170, 114, 70 ° Measured at high resolution: 536.2876 ° Example 203 Amino acid, [2- [[3- [Cyclopropyl (5,6,7,8,9,10-hexa (please read the note on the back first ^ & then fill in this page)-binding Printed Hydrogen-4-Hydroxy-2-oxy-2-Hydroxy-2-Hydroxyl [b] piperan-3-yl) methyl] phenyl] amino] -1- (R) -methyl-2-oxoethyl]-, 1,1-dimethylethyl ester isolated 0.058 G of the title compound as a white solid. Physical properties are as follows:-MP 122- 1 27 X: (decomposition), XH NMR (CDC13) 5 8.50, 7.60, 7.49, 7.30-7.17, 5.02, 4.31, 3.88, 2.61, 2.46, 1.73, 1.66-1.47, -204-This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm). Printed Chinese Manual for Patent Application No. 83100644 by the Consumer Standards Cooperative of the Central Standard Bureau of the Ministry of Economic Affairs Month) A7 B7 V. Description of the invention (/ ¾ 1.45, 1.42, 0.72, 0.62-0.53, 0.28-0.25 ppm ° 13C NMR (CDC1S) 5 170.8, 165.6, 164.1, 161.3, 142.2, 129.7, 129.6, 123.8, 123.7, 119.0, 118.7, 110.7, 106.0, 50.7, 43.8, 30.7, 29.1, 28.8, 28.2, 26.2, 25.8, 25.7, 22.1, 17.2, 12.9, 5.0, 3.8 PPm〇IR (Hujol) 3297, 2954, 2924, 2855, 1671 , 1611, 1593, 1557, 1488, 1455, 144 ^,-1404, 1393, 1375, 1367, 1249, 1202, 1170, 1070 this minute -1. MS (El) m / z 510, 437, 41〇 366, 339, 311, 172, 146, 57 〇 High resolution found: 5 10.2743. Example 204 Aminocarboxylic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Uran-3-yl) methyl] phenyl] amino] -1 (R)-(1H-oxazol-4-ylmethyl) -2-ketoethyl]-, 1,1-dimethylethyl Ester isolated 0.196 g of the title compound as a white solid. The physical properties are as follows: MP 175-1 79 t: (decomposed). HMR (DHS0) δ 9.90, 7.59, 7.53-7.48, 7.13, 7.05-6.98, 6.81, 4.31, 3.36, -2.94-2.77, 1.85, 1.63, 1.53, 1.36, 1.27, 0.66., 0.40-0.36, 0.1 8, 0.10 pp ffl ° 13C HMR (DMSO) δ 170.4, 159.7, 155.3, 145.3, -205-____ This paper size applies to China National Standard (CNS) A4 (210x297 mm) ---------- Binding Line, 17-1 ". (Please read the note on the back before filling in this page.) Printed by the Chinese Consumer Standards Association of the China Standards Bureau of the Ministry of Economic Affairs No. 83100644 on the revised Chinese manual of the patent application (August 85) Description of the invention (138.5, 134.7, 127.8, 122.7, 118.7, 118.6, 116.9, 116.8, 116. 7, 116.6, 111.1, 105.1, 78. 2, 55.1, 44.6, 30.3, 29.7, 29. 3,28 · 7, 28.2, 26 .0, 25.5, 22.0, 12.7, 6. 6,3.9 ppm0 IR (Nujol) 3260, 3141, 3073, 2925, 2868, 2854, 1679, 1658, 1610, 1592, 15 53 , 1488, 1457, 1444, 1393, 1368, 1343, 1336, 13 22, 1295, 1 276, 1251, 11 6 9 cm_ 1.--MS (EI) m / z 577, 576, 47 7, 110 , 57 〇 Measured value at high resolution: 577. 3058. Example 205 1-Hexahydropyridamine H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl]-Isolated 0.117 g of the title compound as a white solid. Physical properties are as follows: MP 157-1621C (decomposed). NMR (DMS0) δ 10.12, 7.51, 7.42, 7.11, 7.05, 3.35, 2.81, 2.62-2.53, 1.87, 1.61-1.37, 0.61, 0.38-0.32, 0.14, 0, 09 ppm. 13C HHR (DMS0) 5 169.1, 164.5, 160.5, 159.3, 151.0, 138.3, 127.5, 122.5, -118.3, 116.1, 112.0, 104.7, 53.5, 53.0, 44.5, 33.Λ, 30.0, 31.5, 29.1, 28.5, 25 • 8, 25.4, 24.5, 23.0, 22.0, 14.2, 12.6, 6.3, 3.8 ppm. _ ~ /! 0 R -_ This paper size applies the Chinese National Standard (CMS) Α4 size (210 × 297 mm) — .1 I n order line. One: L (Please read the note on the back ^ -tap and then fill in 1 (This page) Patent Application No. 83 100644 Revised Chinese Manual (85 months) A7 ___ B7 5

Description of the invention (A IR (Nu j ο 1) 2992, 2949, 2923, 2854, 1658, 1610 1591, 1557, 148 8, 1 458, 1443, 1 428, 1403, 1 377, 1366, 1353, 1341, 1337 , 1318, 1 295, 1279, 1269, 1 254, 1225, 1210, 11 2 6 cm-1. MS (ΕΙ) π / 2 478, 461, 449, 393, 283, 246, 98, 84 〇High resolution Found: 478.2820. 'Example 206 benzamidine, 4-chloro-cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piperan-3-yl) methyl] phenyl]-~. 0.157 g of the title compound was isolated as a white solid. Physical properties are as follows: MP 2 3 4. 5-2 3 7 · 51: (decomposition). ΑΗ NHR (DMS0) δ 10.38, 10.22, 7.96, 7.73, 7.62, 7.59, 7.21, 7.12, 3.39, 2.55, 1.89-1.82, 1.63, 1.55, 1.45, 1.38, 0.74-0.69, 0.44-0.38, 0-26-0.21 , 0.1 4 -0.09 ppm ° 13C HMR (DHS0) 5 164.2, 163.8, 162.5, 160.1, 144.3, 138.4, 136.1, 133.7, 129.5, 128.3, 127.7, 122.9, 119.6, 117.8, 110.0, 105.8, 44.5, 30.2, 29.0 , 28.5, 25.8, 25.2, 21.7-, 12.4, 6.4, 3.6 ppm. IR (Jujol) 3283, 2954, 29M, 2855, 1674, 1640, 1615, 1596, 1 587, 1557, 1443, 1435, 1404, 1210, 119 6 cm-1. -207-This paper size applies to China National Standard (CNS) 厶 4 ^ grid (210X29 &quot;? mm) Patent Application No. 83100644 Chinese Revised instruction manual (August 85) A7 B7 V. Description of invention (彳 ^) MS (EI) ia / z 477, 448, 338, 139, 111. High resolution measured value: 477. 171 2. Spring Example 207 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl] -benzylamine isolated 0.144 g of the title product as a white solid. The physical properties are as follows: MP 211-212¾ °-1H NMR (CDCU, CD30D) 5 7.53, 7.37, 7.30, 7.20, (Please read the note on the back before filling this page) • Installation. 3.67, 3.43, 2.61, 2. 53 , 1.75, 1.62, 1.45, 0.71 0.51, 0.28 pp in ° 13C NMR (DMS0) δ 169.0, 163.9, 163.4, 160.3, 144.5, 138.8, 136. 2, 129. 2, 128. 3, 128.0, 126. 122.5, 118.4, 116. 6, 110. 2, 106. 0, 44.6, 43.4, 30.3, 29.2, 28.7, 26 • 0, 25.4, 21 .9, 12.5, 6.6,

* 1T 3. 8 p p ° ° IR (Nujol) 3255, 3104, 2954, 2923, 2869, 2854, 1676, 1654, 1618, 1594, 1560, 1455, 1440, 1404, 1 2 1 δ cm-1. MS (El) m / z 458, 457, 340, 264, 247, 91. At high resolution (PAB M + l), the spring value is -458.2308. Example 208 N- [3- [Cyclopropyl (5,6,? · 18,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl]-3-phenyl-2-acrylamide-208-This paper size applies to China National Standard (CNS) A4 (210 × 297 mm) Ministry of Economic Affairs Central Bureau of Standards Consumer Co-operation Du Printing Economy The Ministry of Standards and Technology Bureau of the People's Republic of China printed the patent application No. 83100644 of the Chinese Patent Application Amendment Sheet (Aug. U5, Aug. 5) A7 B7 V. Description of the invention 0.09 3 g of white title product was isolated. The physical properties are as follows: MP 253-254T: 0 XH HMR (CDCls, CD30D) 5 7.54, 7.57, 7.49, 7.31, 7.21, 6.60, 3.49, 2.55, 2.46, 1.68, 1.56, 1.40, 0.68, 0.48, 0.25 ppm0 13C NMR (DMS0) δ 164.1, 163.4, 160.2, 144.7, 139.9, 1 3 δ. 9, 134.9, 129.8, `` 129. 1, 128.1, 127.7 122.7, 122. 6, 118.5, 116. 8,110.2, 105.9, 44.6, 30.4, 29.2, 28.7, 26.0, 2 5.5 '21.9, 12.6, 6.6, 3.8, 0 · 2 ρ ρ si 0 IR (mineral oil) 3080, 2952, 2924, 2855, 1680, 1661, 1644 , 1629, 1611, 1591, 1560, 1460, 1450, 1441, 1434, 1401, 1368, 1216, 1199 cm-1. MS (ΕΙ) 1Β / ζ 469, 439, 338, 276, 263, 131, 103. Measured value at high resolution: 469.2255. Example 209 Ν- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] butylamidine isolated the title product from 0-1 to 48 grams of a white sample. The physical properties are as follows:-MP 222-224Ό ° r · NHR (CDC13, CDaOD) δ 7.52, 7.41, 7.22, 3.56, 2-62, 2.52, 2.33, 1.78-1.44, 1.00, 0.73, 0.54, _; ___- 209 -_ This paper size applies to China National Standard (CNS) Α4 size (210 X 297 mm) (Please read the notice on the back ## fill out this page)-Binding · A7 B7 No. 3100644 Patent Application Revised page of Chinese manual (August 85) 5. Description of invention (&gt; 〇 /) 0.35, 0.27 ppm ° 130 NMR (DHS0) δ 171.3, 164.7, 163.9, 160.1, 143.7, 138.0, 127. 8, 122 .5, 118.7, 117.4, 110.1, 106.0, 44.4, 30.4, 28.8, 28.3, 25.8, 25.2, 21.8, 18.5, 13.3, 12.2, 5.8, 3.3 ppm 〇IR (mineral oil) 3280, 3252, 3226, 3197, 3152, 3102, 3081, 3042, 3023, 2952, 2922, 2868, 2854, 1677, 1654, 1616, 1595, 1561, 1480-,-1458, 1448, 1405, 1377, 1367, 1359, 1218, 1203, 785 cm-1. MS (El) m / z 409, 380, 362 Γ 339, 310, 21 6, 203, please read the note of Φ, and then install 146 〇 High resolution measured value: 409.2244. Example 210 benzamidine, N- [3- (cyclopropyl (5,6,7,8,9,10-hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -4-fluoro-Hydrogenated 0.172 g of the title product as a white solid. The physical properties are as follows: MP 239-240 A. XH NHR (CDCU, CD3OD) δ 7.96, 7.63, 7.55 , 7.29, 7.24, 7.19, 7.17, 3.49, 2.63, 2.56, 1.75, 1.64, 1.48, 0.75, 0.53, 0.30 ppm〇 13C NMR (DMSO) 5 165.7, 164.4, 164.1, 163.4, 160.2, 144.5, 138.6, 131.6 , 130.5, 130.4, 127.8, 123.0, 119.8, 118.0, 115.4, 115.2, 110.2, 106.0, 210 This scale is applicable to the Chinese National Standard Cricket (CMS) A4 specification (210X297 mm) Staffing of the Central Standards Bureau of the Ministry of Economic Affairs Cooperative printed No. 83100644 of the Chinese Patent Application Specification Revised Page (August 85) A7 B7 V. Description of the Invention (8) 44.7, 30.4, 29.2, 28.8, 26.0, 25.4, 21.9, 12.6, 6.6, 3.8 pp hi 0 IR (mineral oil) 3080, 3001, 2954, 2924, 2855, 1 675, 1640, 1616, 1603, 1589, 1554, 1508, 1480, 1453, 1445, 1436, 1402, 1 378, 1370, 1327, 1263, 1228, 1210, 1193, 1183, 1171, 1162 , 1137, 852, 691 cm_ 1 MS (El) ro / z 461, 433, 432, 268, 233, 220, 207 (Please read the notes on the back before filling in this page). Pack. 1 23, 95 〇Measured value at high resolution: 461.2007. _ '' Example 211 benzamidine, H- [3- (cyclopropyl (5, δ, 7, δ, 9,10-hexahydro-4-hydroxy-2-oxy -2 Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] Isolated 0.136 g of the title product. Physical properties are as follows: MP 217 ° ° C 13C HMR (DMS0) 5 165.5, 164.2, 163.4, 160.2, 144.5, 138.8, 135.2, 131.5, 128.4, 127.7, 122.9, .ar Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economy 119.8, 117. 9, 110. 3, 106 • 0, 44.7, 30.4, 29 .2, 28.7, 26.0, 25.5, 21.9, 12.6, 6.7, 3.8 ppm 〇IR (Sulfur oil) 3220, 2997, 2954-, 2923, 2854, 1679, 1640, 1614, 1595, 1578, 1551 „1447, 1432, 1404, 1378, 1368 , 1219, 1202, 1140, 692 cm-1. MS (ΕΙ) β / z 443, 338, 250, 105, 77 〇-211-This paper size is applicable to China National Standard (CNS) M specification (210X297 mm) No. 83100644 Chinese Specification for Amendment of Patent Application (85 August 2007) A7 __B7 V. Description of the invention Printed on the high-resolution spring measured by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs; 443.2094. Example 212 Benzylcarboxamide,} |-[3- (cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) methyl] phenyl]-. 0.092 g of the title compound doped with osmium doped with a white solid. Physical properties are as follows: MP 222-223T: 13C HMR (DMS0) 5 167.3, 164-.0, 163.4, 160.3, 144.6, 139.0, 135.1, 133.3, 130.1, 129.8, 128.4, 128.0, 127.0, 126.4, 125.5, Ah 25.3, 125.1, 122.9, 119.2, 117.3, 110.2, 106.1, 44.7, 30.4, 29.3, 28.8, 26.0 , 25.5, 22.0, 12.6, 6.7, 3.4 ppm® IR (Hujol) 3269, 3081, 2954, 2856, 1675, 1637, 1613 1586, 1554, 1462, 1446, 1439, 1404, 1371, 1220, 1211, 1202, 781 Cm-1. MS (El) ro / z 493, 465, 464, 155, 127. Measured at high resolution: 493.2255. Example 213 Aminocarboxylic acid, [2-[[3- [cyclopropyl ( 5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino]-: 1 -(S)-(1H-oxazol-4-ylmethyl) -2-oneethyl]-, 1,2-dimethylethyl ester (formula 0-2) see 0 Figure 0 ··· in a 25 Ml, two-neck round bottom flask with nitrogen population, add Buying Example 199 title product (0.204 g) dissolved in 5 ml of tetrahydrofuran (THF) ° plus ________ Γ? 1? 2 ----- This paper size applies to China National Standard (CNS) A4 size (210x297 Gongchu :) (Please read the note on the back first Please fill in this page for further information.) Binding. A6 _ B6_ V. Description of the invention (211) Hydroxybenzotriazole (0.207 g) is added, and the solution is stirred at room temperature for 16 hours. The reaction mixture is reduced under reduced pressure. Chromatography on a 30 g silica gel column produces 0.2 55 g of the title compound and OBBT. The mixture is divided between chloroform and saturated sodium bicarbonate. • The organic layer is concentrated to produce 0.221 g of the title compound as a white crystalline solid. Physics The characteristics are as follows: MP 160-165t! (Decomposition). 'H NMR (DHS0) 5 9.88, 7.58, 7.53-7.48, 7.14, 7.05-6.98, 6.81, 4.31, 3.35, 2.94-2.77, 1.85, 1.63, 1.53, 1.42 -1.23, 1.36, 0.67, 0.41-0.37, 0.20, 0.10 ppm ° 13C HMR (DMS0) δ 170.5, 159.7, 155.3, 145.3, 145.0, 138.5, 134.7, 127.8, 122.6, 118.7, 118.6, 116.9, 116.8, 116.7, 116.6, 110.8, 105.4, 78.2, 55.1, 44.7, 30.3, 29.7, 29.3, 28.7, 28.2, 26.0, 25.5. 22.0, 12.6, 6.6, 3.9 ρριη 0 IR ( Hujoi) 3292, 2996, 2952, 2923, 2868, 2855, 1705, 1661, 1660, 1610, 159.2, 1553, 1488. 1459, 1442, 1427, 1393, 1375, 1368, 1342, 1336, 1294, 1280, 1269, 1253, 1231 · 1170 cm-1. MS (El) a / z 56, 577, 576, 477, 340, 110, 57 ° Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page)-Pack. Line. Measured value at high resolution: 577.3Q42. Examples 214 and 215 The method of Example 196 was used, and the formula prepared in Preparation 58 below was -213- This paper uses the national standard (CNS) A4 specification (210X297 mm) No. 83100644 patent application Revised page of Chinese manual (August 85) A7 ---- ------- B7 V. Description of the invention (yv) P-ι compound (see P chart), the following compounds of the present invention can be prepared. Example 214 Aminocarboxylic acid, [3-[[3- [cyclopropyl (2,5,6,7,8,9-hexaargon-4-hydroxy-2-onecycloheptan [b] piperan-3- Methyl) phenyl] amino] -3-methylpropyl]-, 1,1-dimethylethyl ester (formula P-2, of which hST-Ht-BOC-ethimyl) is shown in the P diagram. 0.033 g of the title compound was isolated as a white foamy bark solid. The physical characteristics are as follows: MP 116-122TM decomposition). "... aH HMR (DMS0) δ 9.83, 7.52, 7.47, 7.13, 7.05, 6.84, 3.22-3.16, 2.59-2.50, ~ 2.44, 1.84, 1.73, U59-1.50, 1.37, 1.25, 0.88-0.80, 0.69 -0.63, 0.42 ~ 0.38, 0.20-0.08 ppm ° 13C HMR (DHS0) δ 169.3, 163.0, 162.8, 155.6, 144.6, 138.7, 131,6, 127.8, 122.5, 118.4, 116.6, 113.1, 105.6, 77.7, 44.8, 36.8, 36.6, 33.2, 30.9, 28.3, 26.1, 24.2, 22.5, 12.4, 6.4, 4.0 ppm. IR (Hujol) 3303, 2953, 2919, 2867, 2855, 1666, (Please read the notes on the back first and fill in this page)

Printed by 1611, 1593, 1552, 1513, 1489, 1456, 1406, 1392, 1376, 1367, 1275, 1251, 119 2, 1169, 1138, 1070 cm, 1T, 1T, 1T (El) m / &lt; z 519, 497, 496,-397, 326, 146, 57. Measured value at high resolution: 497.2635. Example 215 Probamide, H- [3- [cyclopropyl (2,5,6,7,8,9-hexahydro-4-hydroxy-2-_cycloheptan [b] piperan-3-yl) A The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83100644 patent application Chinese manual amendment page (August 85) A7 B7 V. Description of invention (w)) Central Bureau of Standards, Ministry of Economic Affairs 018 克 硬。 Printed on the basis of employee consumer cooperatives] phenyl- (Formula P-2 * where iU is indole) See P diagram isolated 0.018 grams of solid. The physical characteristics are as follows: MP 173-176¾. XH HHR (CDCU) § 7.64, 7.49, 7.39, 7.32-7.09, 6.95, 6.48, 6.28, 4.59, 3.87, 2.83, 2.70, 2.46, 1.78, 1.67, 1.33-1.23, 0.72, 0.65-0.52, 0.23 ppm . MS (El) di / 2 496, 367, 325, 324, 172, 144, 130 ° at high resolution Found: 49 6.2369. Example 216 Carbamate * [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) methyl] phenyl] (phenylmethyl) amino] -2-oxoethyl]-, 1, 1,2-dimethylethyl ester (formula Q-2) is shown in the Q diagram. The title compound can be prepared by the method of the above Example 196 and the compound of the formula Q-1 (prepared according to the following Example 242). 0.021 g of the title compound was isolated as a white solid. The physical properties are as follows: MP 92-96 10. XH NHR (CDC13) S 8.48, 7.33, 7.27, 7.18, 6.87, 5.68, 5.18, 4.71, 4.28-4.14, -3.62, 3.12, 2.59, 2.46, 1.76, 1.65, 1.66-1.48, -1.41, 0.87, 0.55- 0.38, 0.00 ppm〇MS (El) m / z 586, 486, 429, 338, 234, 92, 57 ° -215-(Please read the note on the back before filling this page)-Binding. Binding paper size Applicable to China National Standard (CNS) A4 specification (210X 297 mm) Patent No. 83100644. Application (Chinese manual amendment page) (August 85) 5. Description of the invention (M /) Central Standard of the Ministry of Economy 印 Printed by Employee Consumer Cooperative Controlled at high resolution: 586.3044. Preparation of 53 ethyl- (3-aminobenzylbenzyl) methanol (formula R-2) See the R diagram. Follow the general method for the preparation of 49-52, regardless of the identity change, but W ethylphenyl ketone replaces the ring. Propylphenone * gives the title compound. The physical properties are as follows: MP 90-91Ό 〇HMR (CDC13) 5 7.39-7.31 ^,-7.28, 7.27-7.21, 7.02, 6.94, 5.18, 4.52, 2.31, 1.79-1.65, 0.88 ppm 〇 IR (Hujol) 3423, 3252 , 3088, 2959, 2925, 2873, 2856, 1694, 1601, 1565, 1449, 1281, 1258, 1233, 1 1 70, 1059, 1044, 1024, 755, 697 cm-1. Elemental analysis found: C, 71.58; Η, 6.70; Η, 4.80. MS (El) m / z 241, 212, 91. Example 217 Aminocarbamic acid, [3- [1- (5,6,7,8,9,10-hexahydro-4-oxo-2-oxo-2-oxo-cyclooctyl [b] piperan-3- (Propyl) propyl] benzyl]-, phenylmethyl ester, (Formula R-3) See R diagram. Using the procedure of Example 107 and the compound of formula R-2 (prepared from Preparation 53 above) *, the title compound can be prepared. 0.772 g of the title compound was isolated as a pale yellow foam. The physical properties are as follows: f MP 78-83¾ (decomposed). HMR (CDCU) 5 7.38-7.20, 7.12, 6.71, 5.90, --------- install-(Please read the note on the back before completing this I)

The paper size of the 1T line paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm). The printed Chinese manual for the patent application No. 83100644 printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) A7 _ B7 5 Description of the invention (&gt; A) 5.20, 4.31, 2.60, 2.43-2.33, 2.15, 2.05, 1.73), 1 * 70 * 1, 25, 0.98 ppm〇13C HMR (CDCU) 3 165.4, 1 63.8, 161.3, 142.9 , 138.6, 135.8, 130.0, 129.5, 129.4, 128.7, 128.5, 128.3, 128.2, 122.5, 117.6, 117.4, 110.4, 105.9, 67.0, 41.2, 30.6, 29.0, 28.8, 26.1, 25.7, 23.9, 22.0, 12.2 pp in 〇IR (N uj ο 1) 3297, 2954, 2924-, · 2868, 2854, 1734 1697, 1667, 1 668, 1635, 1611, 1596, 1551, 1493, 1.461, 1455, 1 447, 1426, 1405, 1377 , 1 338, 1311, 1 279, 1221, 117 4, 1106, 1085, 1061, 740, 697 cm-1 O MS (El) m / z 461, 417, 370, 194, 91 〇Measured values at high resolution: 461.2210. Example 218 2H-cyclooctyl [b] piperan-2-copper, 3- [l- (3-aminophenyl) propyl] -5,6,7,8,9,; 10-hexahydro-4- Hydroxy- (formula {? -4), see Figure 1 {. In a 100 ml three-necked round bottom flask with a reflux condenser and nitrogen inlet * add 10% Pd / C (0.5 g) to the title compound of Example 217 (0.85 g) in 15 ml cyclohexene and 15 ml absolute ethanol And the mixture was refluxed for 1 hour. The mixture was filtered through a plug, washed with ethanol (EtOH) and concentrated to give 0.57 g of the title compound as a white solid. The physical properties are as follows: MP 70-77 Ϊ: (decomposed). -217-This paper size is applicable to Chinese National Standard (CNS) A4 specification (2 〖〇297297mm） (please read the notice on the back first Heng # 'fill this page) Employee Consumption Cooperation Du printed No. 83100644 Chinese Patent Application Amendment Page (August 85) A7 B7 V. Description of Invention (&gt; +) &quot; H NMR (CDC13) 5 7.20-7.15, 6.82, 6.71 , 6.60, 4.27, 2.60, 2.45-2.33, 2.15-2.05, 2.02-1.90, 1.74, 1.67-1.22, 100 ppm 〇13C HMR (DMSO) δ 164.8, 163.0, 160.5, 145.7, 139.4, 128.9, 119.9, 118.1, 117.6, 110.1, 104.1, 40.9, 30.3, 29.2, 28.7, 25.9, 25.4, 23.3, 21.8, 12.6 ppm ° MS (El) m / z 327,312,298, .284,270,134 〇Measured values at high resolution : 327. 1843. Example 219 Carbamate, [3-[[3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [M piperan- 3-yl) propyl] phenyl] amino] -3-fluorenyl]-, 1,4-dimethylethyl ester (formula R-6) See R diagram. Using the method of Example 196 and the title product of Example 2 18, the title compound can be prepared. Isolated 0.35 g of the title compound as a white solid. The physical properties are as follows: MP 106-1111 (decomposed). HMR (CDCU) 5 8.1 2, 7.54, 7.30-7.1 4, 4.28, 3.45, 2.58, 2.45, 2.16-2.05, 1.72, 1.58-1.43, 0.97 ppm °-13C NMR (CDCU) 5 169.9, 1 * 6 5.4, 161.3, 156,4, 143.0, 138.4, 129.7, 129.3, 123.4, 118.9, 118.6, 110.5, 105.8, 41.3, 37.4, 36.4, 30.7, 29.0, 28.8, _- 218 -_ This paper size applies to Chinese national standard (CNS) M specifications (210'X297 mm) (Please read the note on the back first ^ fill in this page). Packing · Line No. 83100644 Patent Application Modification Chinese Manual Correction Page (August 85) A7 B7 5 Description of the invention (w)) 2 8.3, 26.1, 25.7, 23.9, 22.9, 22.0, Ί 2.7 ppm 0 IR (Hujol) 3306, 2954, 2925, 2870, 2855, 1673, 1611, 1593, 1 555, 1509, 1490 , 1461, 1455, 1445, 1404, 1376, 1 367, 1280, 1249, 1234, 1197, 1171 cm_ 1 0 MS (El) m / z 498, 425, 398, 381, 369, 327, 298, Ministry of Economic Affairs Printed by the Consumer Standards Cooperative of the Central Bureau of Standards. 57. High-resolution measured value: 498.2728. 》 -Example 220 Promethazine, 3-limyl-N- [3- [l- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Y-cyclo Octyl- [b] piperan-3-yl) propyl] phenyl]-* monohydrochloride (formula R-7) is shown in the R diagram. Methanol was added to a mixture of the title product of Example 219 (0.208 g) and etheric HC1 (5 mL) * and the solution was stirred at room temperature for 2 hours. Removal of the solvent under vacuum yielded 0.018 g of the title compound with white foam. The physical properties are as follows: MP 125-130T (decomposed). HMR (DHS0) 5 10.49, 10.11, 7.93, 7.47, 7.34- 6.98, 4.23-4.12, 3.07-2.99, 2.70, 2.61-2.51, 2.17, 2.00, 1, 61, 1.53, 1.43, 1.35, 0.81 ppro. 13C HMR (DMSO) 5 168.0, 164.5, 162.9, 160.2, 144.5, 138.3, 127.8, 122.8, -118.6, 116.6, 109.9, 104.3, 51.6, 34.8, 33.0, 30.rl, 29.0, 28.5, 25.8, 25.2, 23 . 1, 21.7, 12.4 ppm. IR (Hujol) 3235, 3181, 3132, 3050, 2923, 2867, (Please read the precautions on the back before filling ^ 'this page) Binding and binding The paper size applies the Chinese National Standard (CMS) A4 specification (210X297 (Mm) Printed Chinese Manual for Patent Application No. 83100644 by the Consumer Standards Cooperative of the Ministry of Economic Affairs, Amendment Sheet (August 85) V. Description of Invention (n'f) 2855, 2735, 1666, 1631, 16Π. 1595, 1 552, 1 489, 1462, 1445, 1406, 1377, 1260, 1243, 1223, 1200, 1172, 1107 cm-1. Example 221 Sulfametamine, 4-chloro-N- [3- [l- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piperazin-3-yl) propyl] phenyl]-(Formula R-5, where 1U is C1) See R. In a 10-ml single-necked pear flask with a nitrogen population, add the compound of formula R-4 (0.050 g), Trichlorobenzenesulfonyl chloride (0.032 g), and 3 ml of dichloromethane ( CH2CU). Pyridine (24 ml) was added and the reaction mixture was stirred at room temperature for 1 6.5 hours. The crude reaction mixture was chromatographed on a 25 g silica column * to yield 0.057 g of the title compound as a white solid skull. The physical properties are as follows: mp ιοδ-mt ;. XH HMR (DMS0) δ 10 .48, 10 .23, 7.70, 7. 57, 7. 12 7 · 06, 6.99, 6.81, 4. 07-4 .01, 2.57 * 2.54, 2.18- 2. 05, 1.97 -1 .88, 1.63-1 .54, 1.43- 1.36, ο .75 PP m 〇13C NMR (DMSO) δ 164.7, 162.9, 160. 5, 145 • 3, 138.4, 137.7, 137.0, 129 .3, 128.7, 128.5, 123.8, 119.7, 117.9, 110. 0, 104 .2, 41.0,, 30. 6, 29. 2, 28 .8, 25.9, 25.4, 23 .2, 21. 8- , 12. 5 ρ ρ m ° IR (Nujol) 3256, 2954, 2924, 2869, 2854, 1661, 1634, 1559, 1478, 1462, 1407, 1335, 1188, 1167, 1158, 1085, 760 cm-1. -220-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) —--------- installation ------ order ----- J—line (please read first Note on the back # ^ &lt; 苒 fill this page) Revised Chinese Manual for Patent Application No. 83100644 of the Patent Application of the Ministry of Economic Affairs of the Central Bureau of Standards of China (August 1985) A7 _B7 V. Description of Invention MS (El ) m / z 501, 486, 472, 444, 326 '307, 284, 153 〇High resolution measured value: 501.1377. Example 222 Sulfamethoxamine, 4-cyano-N- [3-[[(5,6,7,8,9,10-hexaaza-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piperan-3-yl) propyl] phenyl]-(Formula R-5, where R ^ iCN) is shown in the R diagram. Using the procedure in Example 22, the title compound was prepared. 0.050 g of white solid label: title compound was isolated. The physical properties are as follows: MP 108-11ΐ ° _ NMR (DMS0) δ 10.46, 10.39, 7.98, 7.84, 7.13-7.08, 7.01, 6.83, 4.05-4.00, 2.56-2.54, 2.11-2.07, 1.99-1.86, 1.63-1.53 , 1.43-1.28, 0.74 ppm ° 13C HMR (DMSO) δ 164.7, 162.9, 160.5, 145.4, 143.6, 136.5, 133.4, 128.6, 127.5, 124.2, 120. 118.3, 117.7, 115.3, 110.0, 104.1, 40.9, 30.4, 29.2, 28.8, 25.9, 25. 5, 23. 2, 22.2, 21.8, 12.5 ppm 〇IR (Nujol) 2954, 2924, 2869, 2855, 1667, 1558, 1464, 1405, 1 198, 1 1 82, 1 167 , 1091 cm-1. MS (El) m / z 492, 477, 463,-435, 326, 166, 153, 102 ○ Measured at high resolution spring: 492.171 9. Example 223 N-[3- [Cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy- -221-This paper size applies to China National Standard (CNS) A4 (210X297) Li) (Please read the note on the back before filling this page)

、 1T No. 83100644 Patent Application Revised Chinese Manual Revised Page (August 1985) A7 __ B7 V. Description of Invention (2-oxy-2H-cyclooctyl [b] piran 3-Methyl) methyl] phenyl] -N-ethylurea (Formula S-2, where R: is ethyl) See S diagram. In a trapped 10 ml two-necked flask, ethyl isocyanate (0.021 g) was added dropwise to the compound of formula s_i (prepared in Example 104 above) (0.100 g) in 1 ml under nitrogen. CH3CN. The reaction mixture was stirred at room temperature for 24 hours, and the solid was collected by filtration to give 0.075 g of the title compound. The physical properties are as follows:-,. MP 215¾ (decomposed). NMR (CDC13 &gt;, CD3OD) δ 7.40, 7.18, 7.10, 3.48, 3.23, 2.62, 2.53, 1.74, 1.63, 1.47, 1.15, 0.72, 0.52, 0.29) ρ. Pm. 13C HMR (DMS0) δ 163.9, 163.4, 160.2, 155.2, 144.3, 140.1, 128.0, 120.3, 116.9, 115.2, 110.1, 106.1, 44.7, 34.0, 30.3, 29.2, 28.7, 26.0, 25.4, 21.9, 15.6, 12.6, 6.6, 3.8 ppm〇IR (Hujol) 2954, 2924, 2868, 2853, 1682, 1660, 1631, 1595, 1 562, 1535, 1 461, 1453, 1448, 1 408, 1252, 1220, 1202, 692 cm-1 . MS (El) π / ζ 365, 337, 336, 324, 233, 207, 172. Measured value at high resolution: 411.2293. Example 22 4 N- [3- [cyclopropyl (5,6,7n8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctane [b] piperan-3-yl) Methyl] phenyl] -H-benzyl gland (formula S-2, where R1 = phenyl) See S diagram. _-222 -_ This paper size is applicable to China National Standards (CNS) 8-4 (210X297 mm) (Please read the note on the back # ^ before filling this page)-Binding-Thread No. 83100644 Patent Application Revised page of Chinese manual (August 85) A7 _ B7 V. Description of the invention (The procedure of Example 223 was used to prepare the title compound. 0.197 g of the title compound was isolated as a white solid. The physical properties are as follows: MP 214-215T: ° NMR (CDC13, CD3〇D) δ 7.43, 7.31-7.13, 7.03, 3.47, 2.62, 2.55, 1,75, 1.64, 1.48, 0.73, 0.52, 0.29 Ρ Π Ϊ ° 13C NMR (DMS0) δ 163.9, 3, 160.2 , 152.5, 144.6, 139.8, 139.3, 128.8, 128.1, 121.8, 121.2, 118.1, 117.4, 115. 6, 110 .1, &quot; 106.0, 44.7, 30.3, 29.2, 28.7, 26.0, 25.5 , 22.0, 12.6, 6.6, 3.8 ppm 〇IR (oil mill) 3360, 2953, 2924, 2855, 1660, 1630, 1596, 1562, 1 548, 1446, 1409, 1237, 1220, 1199, (Please read the back Note # ^ 再填 窝 本页)-Packing. Order MS (El) m / z 459, 458, 366, 340, 265, 247, 94 printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. Example 225 [3- [ Propyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] _, benzene Ethyl carbamic acid (Formula T-2, where Ri is phenyl) See T. In a flame-dried 10 ml two-necked flask, under nitrogen and Ot; phenyl chloroformate (0.092 g) was dropped dropwise. Add to a compound of formula T-1 (prepared according to Example 164) (0.200 g) in 2.3 ml ·% pyridine. The reaction mixture was stirred at 0 t for 3.5 hours, added to room temperature and concentrated. The residue was concentrated at 5 Milliliter of toluene was absorbed and concentrated 3 times. Column chromatography was performed on 25 g of silica gel to obtain 0.1 (31 g of the title compound as a white solid. —_—-~ 9 9! ^ — This paper size applies to Chinese national standards (CNS) A4 Specification (2 丨 0X297 mm) Line No. 83 100644 Patent Application Revised Chinese sharp book (August) A7 _ ten B7 V. Description of the invention (0 ya Physical properties are as follows: MP 208-209¾ ( break down). NMR (CDCU) δ 7 .58, 7.43 -7.30, 7.28, 6.54, 3.93, 2.60, 2.44, 1.73, 1. 58- 1.41, 0.78-0 .69, 0.64- 0.52, 0.31-0 .24 ppm 0 13C NMR (CDCU) δ 166.5, 6, 164.1, 161.3, 151.5, 150.4, 142.4, 138 129.8, 129.3, 125.6, 123.3, 121.5, 118. 1,117 • 5, 110 • 7, '' 10 5.9, 43.8, 30.6 , 29.1, 28.7, 26.1, 25 .7, 22.1, 13.0, 5.0, 3.8 ppm 〇IR (mineral oil) 3325, 2951, 2925, 2868, 2854, 1742, 1668, 1654, 1614, 1596, 1559, 1538, 1492 , 1464, 1456, 1439, 1293, 1248, 1228, 1202, 1166, 691 cm ^ 1 〇MS (El) n / z 459, 365, 337, 233, 220, 207, 94 ° (Please read the note on the back first Fill in this page again and again).

.tT Printed by High Consumer Analytical Cooperatives, Central Standards Bureau, Ministry of Economic Affairs, measured value: 45.9205. Example 226 [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl]-, ethyl ester carbamic acid (Formula T-2, where h is ethyl) See T diagram. Using the procedure of Spring Example 225, the title compound can be prepared. 0.186 g of the title compound was isolated as a white sample. The physical properties are as follows: _-HP 162 ¾ ° XH NMR (CDC13) 8 7.48, 7.38, 7.28, 7.15, 6.71, _- 224-_ This paper size applies to the Chinese National Standard (CNS) A4 specification (210x297 Gongchu) No. 83100644 Patent application A7 Chinese manual revision page (August 1985) B7 V. Description of invention (is) 6.50, 4.21, 3.91, 2.61, 2.44, 1.73, 1.57- 1.35, 1.30, 0.74, 0.58, 0.27 ρ Ρ HI ° 13C HMR (CDCls) δ 165.6, 164.1, 161.2, 153.4, 142.3, 138.6, 129.7, 122.7, 117.9, 117.4, 110.7 106.0, 61.61, 43.8, 30. 6, 29. 1, 28 . 8,26. 1,25. 22,0, 14.4, 13.0, 4.9, 3.8 ρ ρ ι π IR (mineral oil) 3293, 3258, 3219, 3207, 3146, 3099, 3.81, 2995, 2954, 2923, 2855 ,-1679, 1647, 1614, 1598, 1558, 1 482, 1 464, 1447, 1440, 1405, 1378, 1368, 1359, 1303, 1251, 1214, 1199, 1187, 1172, (Please read the notes on the back first ¾ Refill this page)-Pack. 1071 cm-1. MS (El) m / z 411, 383, 370, 336, 259, 233, 207, 205, 172, 144. Measured value at high resolution · 41 1 .2056. Example 227 2H-cyclooctyl [b] piperan-2-oxy-5,6,7,8,9,10-hexahydro-4-hydroxy-3- (2-methyl-1-phenylpropyl) )-(Formula U-3) See U figure. Using the procedure described in Example 107 and the title compound of Preparation 54 below, the title compound can be prepared. 0.493 g of the title compound was isolated as a white solid. The physical properties are as follows:-MP 214-216 ^ °-x \ {NHR (CDCU) 5 7.46, 7.32, 7.23, 6.02, 3.94, 2.86-2 / 79, 2.58, 2.47-2.40, 1.73-1.71, 1.59-1.54, ___- 225 -___ This paper size applies to Chinese National Standard (CNS) A4 specification (2! 0X297mm), printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention (224) A6 B6 1.48- 1.46, 1.41-1.39, 0.98, 0.97 ppm. 13C NMR (CDCU) δ 165.3, 163.5, 161.3, 142.2, 129.0, 128.2, 126.8, 110.0, 106, 4, 48.5, 30.8, 29.2, 28.9, 28.3, 26.3, 25.8, 22.2, 22.1, 21.0 ppm «IR (Mujol ) 2955 .2925, 2867, 2δ55, 1658, 1632, 1621, 1541, 1454, 1409, 1211, 1185, 1169 cm. Preparation of 54 2-methyl-phenylphenyl-1 -propanol (Formula U-2) See U nursery. (Please read the precautions on the back before filling this page) The Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs printed a 500-liter three-necked round-bottomed flask with a nitrogen inlet and added isopropyl phenone (7.5 ml) And 90 ml of ethanol. Sodium borohydride (7.6 g) was added in three portions, and the resulting mixture was seeded at 25 t for 5 hours. The reaction mixture was cooled in an ice bath, and 100 ml of 10% hydrochloric acid (HC1) was added dropwise over 1 hour. After stirring for an additional hour, the reaction mixture was extracted with three 100 ml portions of dichloromethane. The organic calendar was combined, dried over magnesium sulfate (MsSO), filtered, and concentrated to give 6.768 g of a colorless oil. Chromatography on a 100 g silica gel column yielded 6.601 g of the title compound as a colorless liquid. aH NMR (CDCU) d 7: 35-7.24, 4.32, 1.98, 1.97-1.91, 0.98 · 0.78 ppm. 13C NMR (CDCU) 5 143.51, 128.0, 127.2, 126.4, 79.9, 35.1, 18.8, 1.8.1 ppb〇IR (neat) 3404, 2960, „2931, 2908, 2894, 2872, 1469, 1453, 1034, 1022, 760, 750, 740, 701 cm_1. -226--Binding: α. Patent Application No. 83100644, Revised Page of Chinese sharp book (August 1985) 5. Description of Invention (: //) Central Standard of the Ministry of Economic Affairs MS (El) m / z 150, 107 '79. 77 printed by the Bureau's Consumer Cooperatives. Example 228 (+)-(1〇-3- (cyclopropylphenylmethyl) -5,6,7,8 , 9,10-Hexahydro-4-hydroxy-2H-cyclo [b] piperazin-2-one Example 107 The title compound was separated by HPLC as described in Example 247, using 2.0 parent 25 cm (^ 31 31006100 is Stationary phase * 4% ethanol and 0.1% ester acid / hexane are mobile phases (16 ml / minute>. The physical properties are as follows: The retention time of the title compound is 24. minutes. Found by elemental analysis: C, 77.34; Η; 7.80 Example 229 (-)-(S) -3- (cyclopropylmethyl) -5,6,7,8,9,10 -hexahydro-4-hydroxy-2H-cyclo [b] piperan-2 -Ketone Example 107 The title compound was isolated as described in Example 228 above. The physical properties are as follows: The retention time of the title compound was 33.6 minutes. Measured by phytochemical analysis: C, 77.74; H, 7.62. Example 230 (1 ^ or 5) -3- (cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-cyclo Hepta [b] piran-2 (5H) The title compound of Spring Example 112 was separated by HPLC * as described in Example 247, using 2. Ox 25 cm Chiral cel 0D as the stationary phase, and 4.5% ethanol and 0.2% acetic acid / hexane Alkane is a mobile phase ([delta] ml / min). The physical properties are as follows: _ The retention time of the title compound is 20.5. Example 231 (R or S) -3- (cyclopropylphenylmethyl) -6, 7,8,9-Tetrahydro • 4-Hydroxy-cycloheptan [b] piperan-2 (5H) -one (Please read the note on the back before filling in this page)-Binding 'The paper size is applicable to China Standard Rate (CNS) A4 Specification (210X297 Gong 1) No. 83100644 Patent Application Chinese Specification Revised Page (August 1985) V. Description of Invention (, &gt; 4 Printed Example 112 of the Consumer Cooperatives of the Central Standards Bureau, Ministry of Economic Affairs The title compound was isolated as described in Example 2 30 above. The physical properties are as follows: The residence time of the title compound is 27.4 minutes. Example 232 3- (R)-(Cyclopropylphenylmethyl) -4-hydroxy-10- (R or S) -propyl-5,6,7,8,9,10-hexahydro-cyclooctyl [b] Piperan-2-one followed the general method of Example 121 without significant changes, but the title compound of Example 228 (0.2δ8 g) was substituted for &-( cyclopropylphenylmethyl) -5, 6 , 7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctane [b] piperan-2-one to obtain 0.085 g of the title compound as a white solid 'The physical properties are as follows: aH NMR (CDC13) 5 7.51, 7.37, 7.29, 6.18, 6.16, 4.05, 3.99, 2.93-2.90, 2.76-2.65, 2.18-2.10, 2.01-1.94, 1.78-1.61, 1.54-1.41, 1.37-1.27, 1.22-1.13, 0.97-0.83, 0.77-0.73, 0.63-0.58, 0.29-0.26 ppm. MS (El) m / z 366, 338, 325, 275, 131, 91. High-resolution prediction: 366.2200. Example 233 3- (R)-(Cyclopropylphenylmethyl) -4-hydroxy-10-U or S) • propyl-5,6,7,8,9,10-hexakis-cyclooctyl [ b] Nan-2-one Example 232 The title compound was separated by HPLC as described in Example 447, using 2.0x25 cm Chiral cel 0D as the stationary phase, and 1.5% ethanol and 0.2% acetic acid / hexane as the mobile phase (16 Ml / min). (Please read the note on the back 4 before filling this page)-Binding · Binding-228 ^ This paper size applies to Chinese National Standard (CNS) A4 specification (2 丨 0X297 mm) No. 83100644 Patent Application Revised pages of the manual (δ5 years in August) V. Description of the invention (&gt; ^ The physical characteristics printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs are as follows: The retention time of the title compound is 16.4 minutes ° Example 234 3-U)-(cyclopropane Methylbenzylmethyl> _4_hydroxy-"— (foot or 5) -propyl-5,6,7,8,9, 10-hexahydro-cyclooctyl [b] piperan-2-one Example 232 title The compounds were isolated as described in Example 233 above. The physical properties are as follows: The retention time of the title compound is 18.2 bis. Example 23 5 3- (S)-(Cyclopropylphenylmethanehydroxyl-10- (R or S) -Propyl-5,6,7,8,9,10-hexahydro-cyclooctyl [b] piperan-2-one follows the method of Example 121 * and has no identifiable changes, but with the title compound of Buying Example 229 ( 0.230 g) of substituted 3- (cyclopropylbenzylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-211-cyclooctano.] Piperan-2 -_ * 0.031 g of the title compound of white solid skull. Physical properties are as follows: &quot; H HMR (CDC 1 3) δ 7.53-7.50, 7.37, 7.29, 6.18, 6.16, 4.05, 3.99, 2.96-2.93, 2.79-2.73, 2.18- 2.10, 2.0, 1.94, 1.78-1.61, 1.43-1.22, 1.19-1.28, 0.97-0.86, 0.78- 0.69, 0.63-0.58, 0.52-0.50, 0.29-0.15 ppm ° MS (El) m / z 366, 338, 325 275, 1 31, 91 ° Measured value at high resolution: 366. 2200. Example 236 3- (S )-(Cyclopropylphenylmethyl) -4-hydroxy-10-U or S) __-229 -__ This paper size applies to China National Standard (CMS) A4 (210X297 mm) (Please read the back first (Note 1 fill this page again).

.1T Line No. 83100644 Patent Application Chinese Specification Revision Page (August 1985) V. Description of Invention (&gt; β) Consumption Cooperation with Employees of the Central Bureau of Standards of the Ministry of Economic Affairs Du-Pr-5,6,7, 8,9, 10-Hexahydro-cyclooctane. [B] Wafer- 2-m Example 235 The title compound was isolated by MHPLC as described in Example 247, using 2.0 parent 25 cm (^ 31 31 06100 as the stationary phase, And 4.5% ethanol and 0.2% acetic acid / hexane are mobile phases (16 ml / min). The physical properties are as follows: The residence time of the title compound is 14.7 minutes. Example 23 7 3-(S)-(cyclopropylphenyl f ) -4-hydroxy-10-(R or S) -propyl-5,6,7,8,9,10-hexahydro-cyclooctyl [b] nanan-2-one ... Example 235 The title compound is as above It was isolated as described in Example 236. The physical properties are as follows: The retention time of the title compound was 20.9 minutes. Example 238 Aminocarboxylic acid * [2-[[3- (R or S)-[cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -2-ketoethyl]-, 1, dimethyl ethyl ester, Example 200 The title compound was isolated by M HPLC as described in Example 247, using 1.0 X 25 cm Whelk-0 I as the stationary phase. 15% ethanol and 0.1% acetic acid / hexane are mobile phases (5 ml / min). The physical properties are as follows:-The retention time of the title compound is 15. (1 minute. Example 239 aminocarboxylic acid, [2- [ [3- (R or S)-[cyclopropyl (5,6,7,8,9,10) -hexahydro-4-hydroxy-2-oxy-2 []-cyclosimbu]] __ -230-(Please read the note on the back # n &lt; then fill out this page). Binding. The paper size of the thread is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83100644 Patent Application Modification Chinese Specification Page (August 85) A7 ____B7 V. Description of the invention (&gt; &gt; $ Consumption cooperation between employees of the Central Bureau of Standards of the Ministry of Economic Affairs, Du-Man-3-yl) methyl] benzyl] limyl] -2- 嗣 B The title compound was isolated as described in Example 238. The physical properties are as follows: The retention time of the title compound is 19.6 minutes. Example 240 Aminocarboxylic acid, [2-[[3 -(R or S)-[cyclopropyl (5,6,7,8.9.10-hexahydro-4-hydroxy'-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl Methyl] benzyl] aminediyl] -imidazol-4-ylmethyl) -2-methylethyl]-, 1,1-dimethylethyl ester Example 213 The title compound is as follows Example 247 isolated as K HPLC, utilizing a parent 25 cm 2.0 (: 1 to ^ 431 ^ &amp; 0 stationary phase and 8% ethanol 0.:196 acetate / hexane as a mobile phase (12 ml / min). The physical properties are as follows: The residence time of the title compound is 125 minutes. Example 241 Aminocarboxylic acid * [2-[[3- (R or S)-[cyclopropyl (5,6,7, 8.9.10- hexahydro-4- meridyl-2-oxy-2H- Cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -1- (S)-(1H-imidazol-4-ylmethyl) -2 -fluorethyl]-, 1, The title compound was isolated as described in Example 240. The physical properties are as follows: The residence time of the title compound is 152 minutes. Spring Example 242 3- [Cyclopropyl- [3-[(phenylmethyl) amino] phenyl] methyl] -5,6,7,8,9,10-hexahydro-4-hydroxy-211 -Cyclooctyl [1]] piperan-2-one (formula BB-2, where 1U2 is benzyl) see BB diagram. -------- ~ 2 31 I ______ This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) (Please read the notes on the back first before filling this page). Binding. Thread Revised Chinese Specification Sheet of Patent Application No. 83100644 for Employees' Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (August 85) A7 B7 V. Description of the Invention (Example 164 Title Product, Formula II-1 (100 mg) and Benzaldehyde / A solution of ethanol (6 ml), refluxed for 30 minutes, cooled, and concentrated under vacuum. The resulting oil was dissolved in methanol (6 ml), treated with sodium cyanoborohydride (15 mg), and stirred at room temperature. After 18 hours, the reaction was stopped in K water, diluted with K ethyl acetate, and the organic layer was washed with water and brine * dried (anhydrous sodium sulfate), tested and concentrated in vacuo. The crude product was chromatographed on silica gel to yield 93 mg of the title compound. , It is white amorphous solid cod. 'The physical properties are as follows:… aH NMR (CDC13) 5 7.1-7.4, 6.88, 6.75, 6.6, 6.37, 4.3, 3.9, 2.6, 2.4, 1.7, 1.2 -1.8, 0.6, 0.2 P pm ° 13C NMR (CDCU) 5 1 66, 164.2, 160.9, 142.4, 138.8, 130.1, 128.5, 127.3, 127.1, 116.2, 112.0, 111.9, 110.8, 106.2, 48.0, 43.6, 30.54, 29.1, 28.7, 26.1, 25.7, 21.9, 12.8, 4.6, 3.7 ppm.MS (EI): 429, 338, 303, 277, 236, 222, 209, 144, 132, 91. HRMS: 429.2309 〇 TLC (silicone GF): Rf = 0.24 40% ethyl acetate / hexane. Example 243 3- [cyclopropyl- [3-[(2-phenylethyl) Amine] phenyl] methyl] -5,6,7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperan-2-fluorene (formula BB-2, where Aβ2 (Phenylethyl) See figure BB. Using a method similar to Example 242 * Can be taken from Example 164 and benzyl acetaldehyde -232-This paper size applies to China National Standard (CNS) A4 specification (210 ×: 297 mm) ) (Please read the note on the back 14 &lt; fill in this page first)-Install · Printed Chinese Manual of Patent Application No. 83100644 by the Consumer Standards of the Central Standards Bureau of the Ministry of Economic Affairs Amendment Page of Chinese Manual for Patent Application (δδ 1985) A7 B7 5 Description of the invention (ef) The title compound is prepared. The physical properties are as follows: White amorphous solid. ^ NMR (CDC13) § 7.1-7.4, 6.9, 6.7, 6.5, 6.4, 3.9, 3.4, 2.9 &gt; 2.6 »2.4, 1.2 ~ 1.7, 0.6, 0.25 ppdi ° HS (EI): 443, 352, 200, 158 , 143, 130, 117, 105, 91, 55 ° HRMS: 443.2460 ° .. TLC (silicone GF): Rf = 0.24 40% ethyl acetate / hexane. Example 244 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -N- (phenylmethyl) -benzenesulfonamide (Formula BB-3, where Rβl is phenyl and Re2 is benzyl) see BB diagram. Example 242 A solution of the title product (30 mg), sulfenyl chloride (9 µl) and pyridine (20 µl) in dichloromethane (2 ml) was stirred at room temperature for 18 hours. The solution was diluted with ethyl acetate, washed with water and brine, dried (anhydrous sodium sulfate), filtered, and concentrated in vacuo. Chromatography on silica gel yielded 32. mg of the title compound as a white amorphous solid. The physical properties are as follows: aH HHR (CDCU) 5 7.6, 7.5, 7.2-7.3, 7.0, 6.9, 6.2, 4.7, 3.8, 2.6, 2.4, 1.7-, 1.1-1.8, 1.1, 0.5, 0.40, 0.04 ppw〇 «13C HHR (CDC13) 5 166, 164, 160, 142, 139, 138, 135, 132, 129, 128.8, 128.5, 128.3, 127.9, 127.5, _______-___ This paper size applies to China National Standard (CNS) A4 specifications (210X297 (Mm) (Please read the notes on the back of the page before filling in this page) Binding · * Revised the Chinese Patent Application No. 83100644 revision page (August 85) A7 B7 V. Description of the invention (&gt; 5 Points 111, 106, 55, 43, 30.5, 29.0, 28.7, 26.1, 25.7, 21.9, 12.8, 4.6, 3.7 ppm ° MS (EI): 569, 541, 428, 302, 276, 234, 207, 91, 44 0 HRHS: 569.2227 ° TLC (silicone GF): Rf = 0.38 40% ethyl acetate / hexane. Spring example 245 N- [3-[cyclopropyl (5,6,7,8,9,10-hexahydro -4-Hydroxy-2-oxy_2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl J_-N- (phenylmethyl) -methanesulfonyl pamine (Formula B & -3 * Wherein Rβl is methyl and Re2 is benzyl. See the BB diagram, using a similar method to the title compound starting from Example 243 and methanesulfonyl chloride, but The title compound is prepared. The physical properties are as follows: White amorphous solid. MS (EI): 507, 479, 428, 302, 276, 233, 220, 207, 91 〇HRHS: 507. 2070 〇TLC (silicone GF):! U = 0.10 40% ethyl acetate | Purpose / Hexane. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. Example 246 N- [3- [cyclopropyl (5,6,7, δ, 9,10-hexagon- 4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -H- (2-benzylethyl) -benzenesulfonamide (formula BB-3 * Wherein Rβl is benzylethyl and Re2 phenyl) see BB diagram. Using the similar steps above, but starting from Example 243 title compound and benzamidine chloride * The title compound can be prepared. __________; --22Λ ~ = This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83 100644 Patent Application Revised Chinese Manual (August 85) A7 B7 Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (4¾ The physical properties are as follows: White amorphous solid. MS (EI): 583, 492, 442, 351, 322, 158, 143, 91, 77 ° HRMS: 583.2398 〇 TLC (silicone GF): Rf = 0.22 40% ethyl acetate / hexane. Example 247 (-)-3-[(3-Benzyloxycarbonylaminophenyl) cyclopropylmethyl] -5,6,7,8,9,10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperan-2-one (formula AA-2); "and (+)-3-[(3-benzyloxycarbonylaminobenzyl) cyclopropylmethyl] 6,7,8,9, 10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperan-2-one (formula AA-5) is shown in the AA chart. Example 119 Stock solution of the title compound (9 mg / ml) in 35% isopropanol / hexane * at 1.0 x 25 cm (R, R) Whelk-0 1 (Regis, T ech η ο 1 ogies, I nc. , M rot n Grove, IL 6 0 5 3) on a column to chromatographically using an automatic chromatography system at 5 ml per injection. The eluate * was tracked at 310 nm * and the appropriate fractions were mixed under multiple injections * vacuum concentration to produce a snow-white solid. Fractions obtained from multiple injections were analyzed on a 0.46 X 25 cm U, R) Whelk-0 1 column. The same solvent was used at 1.0 ml / min. The first peak obtained from a 1.0 cm column is: 15.1 minutes * k = 3.03 in a 0.46 cm column, [α] = + 49β (c = 3.6 g / ml methanol), &gt; 95% purity "in the latter peak For 5U 26.5 minutes, k = 5.64, α = 1.86 in 0.46 cm column r, [α] = -49. (C = 3.1 g / ml methanol), &gt; 95% purity. Example 248 (-)-3-[[Cyclopropyl- [3-amino] phenyl] methyl (Please read the notes on the back first ¾ and then fill out this page) • Packing. Thread-This paper size is applicable Chinese National Standard (CNS) A4 specification (210 X 297 mm) No. 83 100644 Chinese explanation of patent application 蓍 revised page (§5 years δ month) V. Description of invention () Office of the Central Procurement Bureau of the Ministry of Economic Affairs Consumer Cooperatives Printed 5,6,7,8,9,10-hexahydro-4-hydrocarbyl-2H-cyclooctyl [b] piperan-2-_ (Formula AA-3) See AA diagram. Example 247 A mixture of the title compound (650 mg) and 10%? 0 | / (: (350 mg) in cyclohexyl fluoride (25 ml), heated at 100 t for 4 hours, cooled, and EtOAc ( (50 ml), diluted with celite, washed with ethyl acetate. The mixed filtrate was concentrated in vacuo and chromatographed on silica gel to produce 366 mg of the title compound as a white amorphous solid skeleton. The physical properties are as follows : _ .NMR (CDC13) 5 7.2, 7.0, 6.8, 6.6, 3.8, 2.6, 2.4, 1.8, 1.2-1.6, 0.7, 0.6, 0.3 ppm ° TLC (Sand GF): 1 = 03640% ethyl acetate / Hexane. [Ot] = -65 ° (c = 0.006 g / ml methanol), &gt; 95 purity. Example 249 (+)-3-[[cyclopropyl- [3-amino] benzene [Methyl] methyl] -5,6,7,8,9,10-hexahydro-4-hydroxy-211-cyclooctyl [1]] piran-2-fluorene (formula AA-6) See AA diagram. Example 248 A mixture of the title compound (800 mg) and 10% Pd / C (400 mg) in cyclohexene (25 ml), heated to 100 ° C for 4 hours, and cooled and diluted with ethyl acetate (50 ml). 2. Pass through Sairi and wash the dike with ethyl acetate. The combined filtrate was concentrated in vacuo and chromatographed on silica to yield 460 mg of the title compound as a white amorphous solid. The physical properties are as follows: _ HMR (CDC13) 8 7.2, 7.0, ^ 6.8, 6.6, 3.8, 2.6, 2.4, 1.8, 1.2-1.6, 0.7, 0.6, 0.3 ppm. TLC (silicone GF): Rf = 〇.i6 40 % Ethyl acetate / hexane. ---------- Private clothing-(Please read the notes on the back ^. 'Before filling this page), 11-line paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) ) No. 83100644 Patent Application Revised Chinese Revision Book (August 85) V. Description of Invention (&gt; M) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs [Of] = + 67 ° (c = 0.0016 ^ / Ml methanol), &gt; 95 purity. Example 250 (-)-4-Chloro-fluorene-υ-ί: Cyclopropyl (5,6,7,8,9,10-hexahydro-4- meridyl-2-oxy-2fluorene-cyclooctyl [ b] pyridin-3-yl) methyl] benzyl] -sulfenylamine (Formula AA-4, where Re. is 4-chlorophenyl) See AA diagram. Example 248 A solution of the title compound (50 mg), pyridine (25 µl), and 4-chlorobenzenesulfenyl chloride (33 mg) in dichloromethane (3 ml) was stirred at room temperature for 18 hours. The crude reaction mixture was chromatographed on a silica gel to give 53 mg of the title compound as a white amorphous solid. A portion of the product crystallized from dichloromethane and hexane. ^ Physical properties are as follows: aH NMR (CDC13) 5 7.6, 7.4, 7.2, 7.1, 7.0, 6.5, 3.8, 2.δ, 2.5, 1.3-1.8, 0.7, 0.6, 0.4, 0.15 ppm. 13C NMR (CDCU) 6 166, 164.4, 161.6, 143.1, 139.4, 138, 136.8, 129.8, 129.2, 128.7, 125.1, 121.1, 120.3, 110.8, 105.9, 44.0, 30.8, 29.2, 28.9, 26.2, 25.8, 22.2, 12.9, 4.6, 3.7 ppm. TLC (silicone GF): Rf = 0.18 40% ethyl acetate / hexane. Example 251 (+)-4-chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Pyridin-3-yl) methyl] phenyl] -benzenesulfonamide (Formula Α-7, where 4-chlorophenyl) is shown in the AA diagram. «-Example 249 A solution of the title compound (50 mg), pyridine (25 µl), and 4-chlorobenzenesulfonyl chloride (33 mg) in dichloromethane (3 ml) * at room temperature -237-__ ( Please read the note on the back ^ 6 before filling out this page) -Pack. 、 -Ιτ -Line-This paper size is applicable to China National Standard (CNS) A4 specification (210X297mm) No. 83100644 Patent Application Chinese Specification Correction Page (August 85) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. The crude reaction mixture was chromatographed on silica to give 63 mg of the title compound as a white amorphous solid. The physical properties are as follows: NMR (CDC13) 5 7.6, 7.4, 7.2, 7.1, 7.0, 6.5, 3.8, 2.6, 2.5, 1.3-1.8, 0.7, 0.6, 0.4, 0.15 ppm. Ding Ding (: (silicone 0 卩): ^ = 0.18 40% ethyl acetate / hexane. [A] = + 28 ° (c = 0.00 ig / ml formazan), &gt; 95% blunt Degree. Example 252 (-)-1 [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl. [&Gt; 1 Naran-3-yl) methyl] phenyl] -4-fluoro-benzenesulfonamide (Formula AA-4, where Re0 is 4-fluorophenyl) See AA diagram. Example 248 Title product (50 mg), A solution of pyridine (25 µl) and 4-fluorobenzenesulfonyl chloride (34 mg) in dichloromethane (3 ml) was stirred at room temperature for 18 hours. The crude reaction mixture was chromatographed on silica gel. 55 mg of the title compound can be produced as a white amorphous solid. Physical properties are as follows: HP 204-206¾ OM NMR (CDC13) 5 7.7, '6'9-7.3, 3.8, 2.6, 2.4, 1.7, 1.3-1.δ , 0.7, 0.6, 0.4, 0.1. TLC (silicone GF): Rf = 0.19 40¾ ethyl acetate / hexane. [Ct] =-6 6 ° (c = 0.0019 g / ml methanol), &gt; 95% inertness Example 253 (· 〇-Η- [3- [cyclopropyl (-5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl Jb] piperan -3-yl) methyl] phenyl] -4-fluoro-benzenesulfonamide (formula AA-7 * Among them Reo is 4-fluoro-238- This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) (Please read the notes on the back first, and then fill out this page) • Packing. -Δ Line No. 831 00644 No. H in patent application ... Netbook revision page (August 85) 5

........................ Ό I V. Description of the invention () 0) Phenyl) See AA diagram. Example 249 A solution of the title product (50 mg), pyridine (25 µl), and 4-fluorobenzenesulfonyl chloride (34 mg) in dichloromethane (3 ml) was stirred at room temperature for 18 hours. The crude reaction mixture was chromatographed on silica gel to give 50 mg of the title compound as a white amorphous solid. The physical properties are as follows: XH NHR (CDC13) 5 7.7, 6.9-7.3, 3.8, 2.6, 2.4, 1.7, 1.3-1.6, 0.7, 0.6, 0.4, 0.1 〇TLC (silicone GF): Rf = 0.19 40 ¾ ethyl acetate / Hexane. [ex] = + 68. (C = 0.0020 g / milliformate), &gt; 95% purity. Example 254 (-)-N- [3- [cyclopropyl (5-, S, 7,3, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooct-3-yl) Methyl] phenyl] -1-methyl-1H-imidazole-4-sulfonamide (Formula AA-4, where Reo is 1-methyl-1H-imidazole) See Figure AA. Example 248 Title product (50 mg ), Pyridine (25 microliters), and methylmethyloxazole-3-sulfosulfonyl chloride (30 mg) in dichloromethane (3 ml), and stirred at room temperature for 18 hours. The crude reaction mixture was on silicone Chromatography to produce 62 mg of the title compound as a white amorphous solid. The physical characteristics are as follows: Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) ) a 7.7, 6.9-7.3, 3,8, 2.6, 2.4, 1.7, 1.3-1.δ, 0.7, 0.6, 0.4, 0.1. TLC (silicone GF): Rf = 0.11 50% ethyl acetate / hexane. Example 255 (-)-4-cyano-N- [3- [cyclopropyl (5.6,7,3,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) methyl-239- This paper size is applicable to Chinese National Standard (CNS) A4 (210XM7 mm) No. 831 00644 Chinese Application for Correction Sheet of Patent Application (85 August A7 B7 group] phenyl] -phenylsulfonamide (formula AA-4, where Re0 is 4-cyanophenyl) see AA chart. Example 248 titled product (66 mg), pyridine (32 μl), A solution of 4-cyanobenzylsulfonium chloride (45 mg) in dichloromethane (4 ml) was stirred at room temperature for 18 hours. The crude reaction mixture was analyzed on silica gel using 50% ethyl acetate / hexane. Alkane can produce 75 g of the title gadolinium b compound, which is a white amorphous solid. The physical characteristics of the printing of the Central Samples Bureau of the Ministry of Economic Affairs, Shellfish Consumer Cooperative, are as follows: MS (EI): 504, 475, 338, 310, 233 153 , 144, 130, 117, 102, 91; 55 ° HRMS: 504'1715.… TLC (silicone GF): Rf = 0.4 (5% methanol / _ imitation). ^ NMR (CDC13) 5 7.85-7.82, 7.75- 7.69, 7.35, 7.19-7.11, 6.95-6.93, 3.47-3.43, 2.64-2.59, 2.55-2.51, 1.73-1.62, 1.46-1.26, .63-.61, .51-.48, .26-, 23, .15-.llppm 0 [α] -87 ° (c = 0.24 methanol). Example 256 (-)-Bu [3- [Cyclopropyl'yl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] pyran- 3-yl) methyl] phenyl] -8-quinolinesulfonamide (Formula AA-4, where Reo is 8-quinolinyl) See AA diagram. Example 248 A solution of the title product (66 mmol), pyridine (32 μl), and 8-quinolinesulfonyl chloride (50 mg) in dichloromethane (4 mL), stirred at room temperature for 72 hours . The crude reaction mixture is chromatographed on silica gel, starting from 50% ethyl 207, 195. 186, (please read the note on the back f-'Tf before filling in the purchase). 、 · Ιτ 线 -240 This paper size is applicable Chinese National Standard {CNS) A4 Specification (210X 297 mm) Patent Application No. 83100644 _ A7 "Chinese Manual Correction Page (August 85) B7 V. Description of the Invention (Ethyl Ethyl Acetate / hexane, followed by 100% ethyl acetate to produce 74 mg of the title compound as a white amorphous solid. Physical properties are as follows: MS (EI): 530, 513, 501, 489, 338 · 310, 298, 233, • 186, 158, 144 , 129, 106, 77, 55, 41 ° HRMS: 530.1889 〇 (Please read the cautions on the back before filling out this page). Equipment. Central Standard of the Ministry of Economics 实例 Printed Example of Employee Consumer Cooperatives 2 5 7-2 5 δ Use The method of class M, example 256, and the following compounds of the present invention can be prepared using a suitable sulfonase [Example. 257 (-)-1 &lt;-[3- [cyclopropyl (5,6,7,8,9 , 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-[(E) '] -ethane Sulfasamine (Formula AA-4, where Re0 is 2-benzene -[E] vinyl) see AA chart. Physical properties are as follows: White amorphous solid. MS (EI): 505, 477, 441, 3-38, 310, 248, 233, 207, 195, 186, 144, 132 , 117, 103〇HRMS: 505.1924 ° -241- Order_line_ TLC (silicone GF): Rr = 0.7 in ethyl acetate. XH HHR (CDCU) δ 8.31 -8.25, 8.02-7.99, 7.62- 7.52. 7.10- 6.95, 3 .71-3 .68, 2. 61-2.57, 2,, 42-2.38, 1.73, 1.54-1.43, 1.25-1 .12 ,. 97-.85, .47- -.44, .32-. 29, -.09-- .11 0 a- [α] -18 ° (c = 0.16 methanol) 0 This paper size applies to China National Standard (CNS) A4 (210X297 mm) Article 831 Patent application No. 00644 A 7 Revised Chinese manual (August 85) B7 V. Description of the invention (^ TLC (silicone GF): Rr = 0.4 (5% methanol / chloroform) ° Example 258 (-卜卜[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-mercapto-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Benzyl] -benzenesulfenamide (Formula AA-4, where Reo is Benzyl) see AA chart 〇 * Physical properties are as follows: White, non-crystalline solid bet. NMR (CDC1S) 5 7.76-7.73, 7.52-7.41, 7.17. 6.99, 3.83, 3.80, 2.61, 2.46, 1.74, 1.58, 1.42, 0.6-0.5, 0.42, 0 · 2ρρπ. 'TLC (silicone GF): Rf = 0.4 (50% ethyl acetate / hexane) ° Example 259 (+)-4-cyano-N- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (formula AA-7, where (4-cyanophenyl). See AA chart. Example 249 A solution of the title product (66 mg), pyridine (32 µl), and 4-cyanobenzenesulfonium (45 mg) in dichloromethane (U ml) was stirred at room temperature for 18 hours. The crude reaction tumor compound was analyzed on silica gel, and K 50% ethyl acetate / hexane yielded 72 mg of the title compound as a white amorphous solid. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economics {Please read the precautions on the back before filling this page) The physical characteristics are as follows: White non-crystalline solid. _ HR MS * · 504.170 ° HS (EI): 504, 476, 338, 310, 233, 220, 207, 195, -242- This paper size applies Chinese National Standard (CNS) A4g (210X297 mm) Central Ministry of Economic Affairs Standard Bureau employee consumer cooperative printed No. 83100644 patent application _ _ A7 Chinese manual revision page (August 85) B7 V. Description of invention (W /) 186. 153, 144, 130, 117, 102, 55 ° TLC (Silicone GF): Rf = 0.4 (5% methanol / aqueous). XH HHR (CDC13) S 7.85-7.82, 7.75-7.69, 7.35, 7.19-7.11, 6.95-6.93, 3.47-3.43, 2.64-2.59, 2.55- 2.51, 1.73-1.62, 1.46-1.26, .63-.61, .51-.48. .26-.23, .15-.11 ppm0 Example 2 6 0-2 6 1 Using the class method in Example 259 and using the appropriate sulphur brewing chlorine, other K Compound. Example 260 (+)-Bu [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3 -Methyl) methyl] phenyl] -8-pyridinosulfonamidate (Formula AA-7, where 1U is 8-quinolinyl) See AA diagram. The physical properties are as follows: White amorphous solid. TLC (silicone GF): Rr = 0.7 (100% ethyl acetate). XH NMR (CDC13) 5 8.31-8.25, 8.02-7.99, 7.62- 7.52, 7.10-6.95, 3.71-3: 68, 2.61-2.57, 2.42-2.38, 1.73, 1.54-1.43, 1.25-1.12, .97-. 85, .47-.44, .32-.29, -.09 to -.11 ° Example 261 (+) -H- [3- [cyclopropyl (5,6,7,8,9, 10- Hexahydro-4-hydroxy-2-oxy-2Ηγcyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-[(E)]-¾enesulfonamide (formula AA-7, where Re0 is 2-phenyl- [E] -vinyl) See AA chart. (Please read the cautions on the back before filling this page). Binding · Binding Line -243- This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Chinese Patent Application No. 83100644 .. Correction Sheet of the Specification (August 85) V. Description of the invention (Physical properties are as follows: White amorphous solid. HRHS: 505.1914 ° MS (EI): 505, 477, 441, 338, 310, 233, 220, 207, 195, 186, 144, '130, 117, 103, 77 〇TLC (silicone GF): Rr = 0.4 (5% methanol / chloroform). Example 26 2 4-cyano- N- [3- [Cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-fluorenyl [b] piperan-3-yl) methyl ] j phenyl] -benzenesulfonamide, see Figure Z. Example 164 Title product (660 g of Γ, pyridine (320 μl), and 4-cyano; benzsulfonyl chloride (440 mg) in dichloromethane Rhenium (40 ml) solution was stirred at room temperature for 18 hours. The crude reaction mixture was evaporated to a volume of 5 ml and chromatographed on silica gel using 50% ethyl acetate / hexane to give the title compound (641 Mg) is a white amorphous solid This amorphous solid can be crystallized from propanol: hexane to produce 499 mg. The physical properties are as follows: White solid: mp 1 83-1 85 scoop. Measured value for elemental analysis: C, 6 6.76; H, 5.68; H. 5.38; s,. · ♦ · 6.30. MS (El) t 504, 476, 338, 309, 233, 220, 207, 195, 186. 153, 144, 130, 1 17, 102 ° HRMS: 504.1710ο TLC (silicon GF): 1 = 0.4 in 50% ethyl acetate / hexane. Example 26 3 H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxyl- -244- This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) (Please read the notes on the back ^ # '' Fill in this page). Installation and nailing No. 83100644 Patent Application A7 、 Chinese Speaking_Medical Book Correction Page (August 85) B7 V. Description of the invention (; K〇〇2-oxy-2Η-cyclooctyl [b] manan-3-yl) methyl] phenyl] -8 -Porphyrinsulfonamide, see Figure Z. Example 164 A solution of the titled product (32 mg), pyridine (16 μl), and 8-dantolinylsulfonyl chloride (25 mg) in dichloromethane (2 mL) And stirred at room temperature for 18 hours. The reaction trace compound was chromatographed on silica gel (50% ethyl acetate / hexane first, and then 100% ethyl acetate as the eluent. The title compound (32 mg) was formed as a white amorphous solid. The physical properties are as follows: White crystalline solid · 婿. MS (EI) _: 530, 513, 501, 33 8. 310, 298, 233, 212, 186, 176, 158, 144, 129.91,-55 ° HRMS: 530. 1882 〇 TLC (silicone GF): Rf = 〇 .7 in ethyl acetate. Example 264 4-chloro-N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (Formula Z-3, in which Rel is 4-aerophenyl) See Figure Z. Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Preparation Example 164 The title product (4Q mg)., Pyridine (20 µl), and a solution of 4-chlorobenzenesulfonyl chloride (25 g) in dichloromethane (2 ml), and stirred at room temperature for 18 hours The crude reaction mixture chromatography (silica gel) K yielded the title compound (50 mg) as a white amorphous solid. The physical properties are as follows:-^ NHR (CDC13) 5 7,6, 7.4, 7.2, 7.1, 7.0, 6.5, r -3. 8, 2. 6, 2.5, 1. 3 -1. 8, 0. 7, 0. 6, 0. 4, 0 1 5 p p m ° -245- This paper size is in accordance with Chinese National Standard (CNS) A4% ^ (210X297 mm) A7 B7 No. 83 100644 Patent Application Judging Chinese Manual Correction Page (August 85)

V. Description of the invention (W 13C NMR (CDC13) 5 166, 164.4, 161.6, 143.1, read first, read δ, then 139.4, 138, 136.8, 129.8, 129.2, 128.7, 125.1, 121.1, 120.3, 110.8, 105.9, 44.0 , 30.8, 29.2, 23 · 9, 26.2, 25 · δ, 22'2, 12.9, 4.6, 3.7 ppm. MS (EI): 513, 485, 338, 309, 233, 207, 195, 186, 144, 130 , 117 ° HRMS: 513.1371 ° TLC (silicone GF): Rr = 0.55 in 50% ethyl acetate / cyclohexane. Examples 265-313 The method similar to that of Example 264 was used, and the appropriate sulfonated chlorine was used (see Z Figure), the following additional compounds of the present invention can be prepared. Example 2δ5 Η- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2- 2-oxy-2H- The physical properties of cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- (l,: l-dimethylethyl) benzenesulfonamide are as follows: White amorphous solid, HS (EI) : 535, 507, 338, 310, 233, 207, 185, 144, 117, 91, 55. HRMS: 535.2389 Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 1: 1 (silicone 6 "): 1 ^ = 〇 .32 (40% ethyl acetate / hexane). Example 2δ6 Η- [3- [cyclopropyl (5,6 · 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H - Huanyu [bί waven-3-yl) methyl] phenyl] -2-naphthalenesulfonamide The physical properties are as follows: -246 This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) A7 B7 8310064 Revised page of Chinese Specification for Patent Application No. 4 (August 1985) V. Description of the invention White amorphous solid, MS (EI): 529, 501, 338, 309, 233, 207, 185. 144, (Please read the back first Please note | ^^ Fill in again; write this page) 127. HRMS: 529.1929 TLC (silicone, GF): Rf = 0.13 40% ethyl acetate / hexane. Example 267 N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -4- (trifluoromethyl) -The benzamidine physical properties are as follows: white amorphous solid, MS (EI): 547, 579, 508, 33'8 ', 233, 220, 207, 186. 144 〇HRMS: 547.1637 TLC (silicone, GF): Rf = 0.30, 40% ethyl acetate / hexane. Example 268 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) The physical properties of methyl] phenyl] -4-fluorosulfamidamide are as follows: ';'. White non-crystalline solid photo, MS (EI) printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs: 497. 456, 338, 309, 233. 207, 186, 144, 95 〇HRMS: 497.1606 〇_ TLC (silicone GF): Rf = 0.20, 4 (^% ethyl acetate / hexane. Example 269 3,4-dihydro-H-C3- [ Cyclopropyl (5,6,7,8,9,10-hexahydro-247) This paper size applies to Chinese National Standard (CNS_) A4 specification (210X297 mm) No. 83100644 Patent Application A7 Chinese Manual Correction Page (δ5 Year δ month) B7 V. Description of the invention (with) 4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide The physical properties are as follows : White amorphous solids, HS (EI): 529 ^ 501, 338, 233, 207, 185, 144, 127, 117, 55. HRMS: 529.1930. TLC (silicone GF): = 0.20 · 40% Z acid ethyl Ester / Hexane. Example 270 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] -3-yl) methyl] phenyl] -naphthosulfonamide The mechanical properties are as follows: White amorphous solid, MS (EI): 547, 519, 338, 309, 233, 207, 186, 144, 130, 117. 55 ° HRMS: 547.0979 ° TLC (silicone, GF): Rf = 0.32 , 40% ethyl acetate / hexane. Example 271 2,5-Dichloro-^-[3- [cyclopropyl (5,6,7,8,9,10-Hexahydro Economic Central Bureau of Standards Staff Consumption Printed by the cooperative (please read the notes on the back first and then fill out this page) -4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl> methyl] benzyl] -benzenesulfonate The physical properties of amidine are as follows: White amorphous solid_ HS (EI): 547, 519, 338, 309, 233, 207. 195, 186, «-144, 1 30, 1 17, 91, '55. * 248- This paper size applies to Chinese National Standard (CNS) A4 (210X297 mm) Patent Application No. 83100644 printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs-Chinese Manual Correction Page (δ5yearsδmonths) HRMS: 507.0987 TLC (silicone, GF): Rf = 0.28, 40% ethyl acetate / hexane. Example 272 4-bromo-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-.2-oxy-2H-cyclooctyl [b] piperan -3-yl) methyl] phenyl] -benzenesulfonamide The physical properties are as follows: White amorphous solid MS (EI): 557, 531, 338, 309, 233, 207, 195, 186, 14 4 °-: HRHS: 557.0863 I. TLC (silicone GF): Rf = 0.23, 40% ethyl acetate / hexane. Example 273 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) The physical properties of methyl] phenyl] -4-nitro-benzenesulfonamide are as follows: Pale yellow amorphous solid HS (EI): 524, 507, 495, 338, 309, 233, 220. 207, 185, 153, 14 4, 50 °, HRMS: 524.1612 TLC (silicone GF) ·· = 0. 18 * 40% ethyl acetate / hexane. Example 274 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] mannan-3-yl) form Phenyl] phenyl]-3-nitro-benzenesulfonamide f physical properties are as follows: (Please read the note on the back & fill in this page before filling in this page).

-1T LINE-249- This paper size is applicable to Chinese National Standard (CNS) A · 4 Specification (210X297mm) No. 83100644 Patent Application Chinese Specification Correction Page (δ5 Aug. 5) ..-... 'Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the Invention (^ /) White amorphous solid MS (EI): 524, 507, 496, 338, 233, 220, 207, 144, 50 HRHS: 524.1622 TLC (Sand GF) ': Rf = 0.17, 40% ethyl acetate / hexane. Example 275 N- [3- [Cyclopropyl (5,6 · 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) The physical properties of methyl] phenyl] -4-methoxy-benzenesulfonamide are as follows: White amorphous solid MS (EI): 509, 481, 338, 309-, 233, 207, 171, 144, 1 32, 1 07, 7 7 〇HRMS: 509.1869 ° TLC (silicone GF): Rf = 0.10, 40% ethyl acetate / hexane. Example 276 4-[[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- Methyl) -phenyl] amino] sulfofluorenyl] -benzoic acid The physical properties are as follows: 'White amorphous solid MS (EI): 523, 495, 476, 338, 233, 207, 194, 166, 14 4; 5 50 0 HRMS: 523.1661 〇 TLC (silicone GF): 0.13 40% ethyl acetate / hexane, plus 1% acetic acid. -250- This paper size applies to China National Standard (CNS) A4 (210X297) (%) (Please read the notes on the back and fill in this page first; write this page)-Pack. * 11 Line No. S310064 No. 4 Patent Application Chinese Manual Correction Page (August 1985) V. Description of Invention (^ f) A7 B7 Example of printing by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 277 [Cyclopropyl (5,6. 7, 3,9, 10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) methyl] phenyl]-2.4.6- Trimethyl-benzenesulfonamide The physical properties are as follows: White amorphous' Solid MS (EI): 521, 493, 338. 310 · 233, 207, 186, 144, 132, 119 〇HRMS: 521.2245 ° TLC (silicone, GF): Rr = 0.25 40% ethyl acetate / hexane. Example 278 {(-[3- [cyclopropyl (5,6 , 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2bcycloxin | &gt;] piperan-3-yl) methyl] benzyl]-2.3.4.5.6- five The physical properties of flubensulfonamide are as follows: White amorphous solid MS (EI): 569, 541, 328, 338, 233, 207, 186, 153, 144, 117 〇HRMS: 569.1294 ° Where (: (silicone 〇?) : 1 = 0.3 3 \ 40% ethyl acetate / hexane. Example 279 H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2- 2-oxy The physical properties of -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,4-difluoro-benzenesulfonamide are as follows: _ White amorphous solid β ~-HS (EI): 515, 487, 338, 309, 233, 207, 177, 144, 251- This paper size is applicable to China National Standard (CNS) A4 size (21.0X 297 mm) (Please read the notes on the back ^ before filling in the guest (This page)

-^ ------------ ^ ------ 1T Printed Patent Application No. 83100644 by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) B7 ____- V. Description of the invention (#) 113. 55 ° HRMS: 515.1574 ° TLC (silicone GF): Rr = 0.38 40% ethyl acetate / hexane. Example 280 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2ioxy-2H-cyclooctyl [b] piperan-3-yl) methyl Phenyl] phenyl] -3- (trifluoromethyl) benzylamidine physical properties are as follows: White amorphous solid MS (EI): 547, 519, 338, 309, 233, 207, 144, 130, 117, 55. HRMS: 547. 1641 °, -Jiji (: (silicone 61?): 1 ^ = 0.35 40% ethyl acetate / hexane. Example 231 N- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-. 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-fluoro-benzenesulfonamide It is as follows: White amorphous solid MS (EI): 497, 469, 338: 309, 233, 207. 186, 144. HRHS: 497.1671 〇 TLC (silicone GF): Rf = 0.28, 40% ethyl acetate / hexane. Example 282 4-butoxy-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H_-cyclooctyl [b] piperazine The physical characteristics of lan-3-yl) methyl] phenyl] -benzenesulfonamide are as follows: (Please read the note on the back. ^ Then fill in this page) -Packing_ Binding Line-252- This paper size applies to China National Standard (CNS) A4 Specification (210X297 mm) Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Printed No. 83 100644 Patent Application A7 Chinese Manual Correction Page (δδ, 1985) y_Ⅴ. Description of Invention (2rf) White Amorphous solid MS (EI): 551, 523, 508, 428, 338, 2233, 207, 144, 91 ° HRMS: 551.2347. TLC (silicone GF) ': Rr = 0.43 40% ethyl acetate / hexane. Examples 2 83 «-[3- [cyclopropyl (5,6,7,3,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl The physical properties of the group] phenyl] -5- (dimethylamino) -1-caisulfosamine are as follows: White amorphous solid diMS (EI): 572, 338, 207, Γ8 · 6 ·, 170, 1 54, 144, 91. HRMS: 572. 2349 ° TLC (silicone GF): Rr = 0.35 40% ethyl acetate / hexane. Example 284 3,5-dichloro-N- [3- [cyclopropyl ( 5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-hydroxybenzenesulfonate The physical properties of hydrazine are as follows: White amorphous solid '.. · · MS (EI): 563, 507, 428, 338, 301, 233, 207, 144, 91 〇HRMS: 563.0940 ° TLC (silicone GF): = 0.2ΐ 40% ethyl acetate / hexane. Example 285 2,3-Dichloro-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydror--4-hydroxyl -2-oxy-2H-cyclooctyl [b] piperazin-3-yl) methyl- (please read the note on the back first and then fill in this page) -pack ·, ιτ 线 -253- This paper size Applicable to China National Standard (CNS) Α4 Specification (210X297 mm) No. 83100644 Patent Application Chinese Specification Correction Page August Α7 __ -_ Β7 • ~ &quot; & q uot; &quot; '' ______________ 5. Description of the invention [] Phenylsulfenilamide Physical properties are as follows: White amorphous solid MS (EI): 547, 519, 397, 338, 233, 207, 144, 91, 55 ° 'HRMS: 547.0989 〇 TLC (Sand Rubber GF): Rf = 0.15, 40% ethyl acetate / hexane. Example 28δ [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] 舅 αρ | -3-yl) methyl] benzene Phenyl] -2 ^ (trifluoromethyl) -toluenesulfonamide physical properties are as follows: ―One Two— · White amorphous solid MS (EI): 547, 519, 338, 233, 207, 186, 144, 91, 55 o HRMS: 547.1654 o TLC (silicone GF): Rf = 0.12 40% ethyl acetate / hexane. Example 287 2-Chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2_oxy_2Η_ · cyclo 芊 [b] piperan- The physical properties of 3-yl) methyl] phenyl] -6-methylbenzylamidine are as follows: Printed by the Consumers Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, a white amorphous solid HS (EI): 527, 499, 33δ, 233 , 207, 186, 144, 125, 91, 49. HRMS: 527.1544 〇-254- This paper size applies to Chinese national standard (CNS> A4 size (21〇 &gt; &lt; 297 mm). The Central Consumers Bureau of the Ministry of Economic Affairs printed a patent application No. 83100644 of the Consumer Cooperatives. — Revised page of Chinese manual (August 85) B7 V. Description of invention (rC3) TLC (silicone GF): Rf = 0.15 40% ethyl acetate / hexane. Example 288 3,5-Dichloro-N- [3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -The physical properties of benzsulfonamide are as follows: White amorphous solid MS (EI): 547, 519, 338, 233, 207, 144, 130, 1 17, 55 〇HRMS: 547.0973 ° TLC (silicone GF): Rr = 0.23 40% ethyl acetate / hexane. Example 2 8 9 3 -Ano-N-[3-[cyclopropane-based C5, 6,7,8,9,10 -hexahydro-4-hydroxy-2-oxy The physical properties of -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide are as follows: White amorphous solid MS (EI): 513, 485, 338, 233, 207, 186 , 144, 130, 111, 55 〇HRMS: 513.1377, where (: (silicone 0?): 1 ^ = 0.17, 40% ethyl acetate / hexane. Example 290 N- [3- [cyclopropyl (5, 6,7,8,9,10 -Hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-benzofurazolamide physical properties are as follows: white Crystal solid (please read the precautions on the back before filling this page)

'1T Line-255- This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297mm) No. 83100644 Patent Application Chinese Manual Correction Page (August 85) 5. Description of the invention (&gt; broken) MS ( EI): 521, 493, 338, 233, 220, 207, 145, 84, 55 ° HRMS: 521.1608. TLC (silicone GF): Rr = 0.12 40% ethyl acetate / hexane. Example 291 3-^-[{-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy | yl-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) methyl] phenyl] -benzenesulfonamide The physical properties are as follows: White amorphous solid MS (EI): 557, 529, 338, 30: 9, 233 · 207, 186, 157, 144, 130.91 , 55. — HRMS: 557.0885. TLC (silicone, GF): 1 = 0.15 40% ethyl acetate / hexane β Example 292 3-[[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- The physical properties of hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfonamido] benzoic acid are as follows: | White amorphous solid 'Central Standard of the Ministry of Economy Printed by the Bureau's Consumer Cooperatives ---------- Install-{Please read the note on the back '^ before filling this page) Line MS (EI): 523. 495, 476, 338, 233, 207 , 194. 166, 144, 121, 55 ° HRMS: 523.1671 ° TLC (silicone, GF): Rr = 0, 15 40% ethyl acetate / hexane plus 1% acetic acid. r ~ Example 29 3 2-Chloro-hydrazone- [3- [cyclopropyl (5,6, 7, 8, 9, 10-hexahydro-4-hydroxy-25 6- ) Α4 specification (210 × 297 mm) Revised Chinese Manual for Patent Application No. 83100644 printed by the Consumer Standards Cooperative of the Ministry of Economic Affairs of the Central Government (85 months § month) A7 ~-B7 V. Description of the invention The physical properties of oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenylsulfenylsulfonamide are as follows: White amorphous solid MS (EI): 513, 485, 338, 233, 207, 186, 144, 130, 111, 91, 55 ° HRMS: 513.1371 〇TLC (silicone 'GF): Rf = 0.1840% ethyl acetate / hexane. Example 294 5-chloro-H- [3- [cyclopropyl ( 5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenylb 1,3-dimethyl The physical properties of oxazole-4-sulfonamide are as follows: White amorphous solid MS (EI): 531, 503, 338, 233, 207, 193, 144, 130, 117, 55 〇HRMS: 531.1608 ° TLC (silicone, GF ): Rf = 0.10 40% ethyl acetate / hexane. Example 295 2,6-Dichloro-N- [3 '-[cyclopropyl (5,6,7,8,9,10-hexahydro-4) -Hydroxy-2-oxy-2H-cyclooctyl [b] piperazine -3-yl) methyl] phenyl] -benzenesulfonamide physical properties are as follows: white amorphous solid_ HS (EI): 547, 519, 338, 310, 233, 207, 144, 84, r- 55 ° -257-This paper size applies to China National Standard (CNS) A4 (210X297 mm) '' Binding ^ / w service (please read the precautions on the back before filling this page) Employees of the Central Standards Bureau of the Ministry of Economic Affairs Cooperative printed the revised Chinese specification of Patent Application No. 83100644 (August 1985) A7 '------------- B7. V. Description of Invention (outside) HRMS: 547.0997 〇TLC ( Silicone, GF): Rf = 0.20, 40% ethyl acetate / hexane. Example 296 H-[[5-[[[((cyclopropyl (5,6,7,8,9,10-hexahydro) -4-Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl '] aminosulfonyl] -2 -thienyl] methyl] benzidine The characteristics are as follows: White amorphous solid MS (FAB): 6 19, 434, 338, 1 1 8, 105 〇HRMS: 619.1926 +. TLC (silicone GF): Rr = 0.65, 50% ethyl acetate / dichloromethane. Example 297 N- [3- [Cyclopropyl (5U, 8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooct-3-yl) methyl] phenyl] -1- The physical properties of methyl- (S) -1H-oxazole-4-sulfonamide are as follows: White amorphous solid MS (EI): 483, 454, 338, 251, 212, 186, 144, 132. HRMS: 483.181 8 〇 TLC (silicone, GF) · R ^ = 0. Ϊ 1 50% ethyl acetate / hexane. Example 298 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan: -3- (Methyl) benzyl] -4- (phenylsulfonyl) -2-thiophenesulfonamide The physical properties are as follows: _ White amorphous solid MS (FAB): 626, 391, 338, 207, 149, 118 , 57 ° -258- This paper size applies to Chinese National Standard (CNS) Α4 size (210X297 mm) ^ --------- ΊΙ-^-I (Please read the note on the back first ^ 孓(Fill in this page again)

'1T Line No. 83100644 Patent Application Case Revised Chinese Manual (August 1985)

Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs HRMS: .626.1359 ° TLC (silicone GF): Rf = 0.10 40% ethyl acetate / hexane. Example 299 [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] p-ranan-3-yl) The characteristics of methyl] phenyl] -5- (phenylsulfonyl) -2-thiophenesulfonamide are as follows: White amorphous solid MS (FAB): 626, 338, 207,195, 144, 118, 55. HRHS: 626.1347. TLC (silicone GF): = 0.124 beta ethyl acetate / hexane. Example 300 [3- [Cyclopropyl (5 ~ «~ 6 _ ;. 7,8,9,10-Hexa-4--4-yl- 2-oxy-2H-cyclooctyl [b] piperan-3 -Methyl) methyl] phenyl] -4-hydrazone-toluenesulfonamide physical properties are as follows: White amorphous solid MS (EI): 605, 338, 207,194, 144, 118, 91, 55. HRHS: 605.0763 ° TLC (silicone GF): Rf = 0.21 '40% ethyl acetate / hexane. Example 301.5 5-Homo-H- [3- [cyclopropyl (5,6, '7,8,9,10-hexahydro-4-mercapto-2-oxy-2H-cyclooctyl [b] i Piperan-3-yl) methyl] phenyl] -2-thiophenesulfonamide The physical properties are as follows: _ White amorphous solid MS (EI): 519, 338, 310, 270, 207, 144, 118, 91 , 259- This paper size is in accordance with Chinese National Standard (CNS) A4 (210 X 297 mm) (Please read the notes on the back 孓 before writing this page)-Packing. Threading Staff Consumer Cooperatives, Central Standards Bureau, Ministry of Economic Affairs Printed the revised Chinese specification of Patent Application No. 83100644 (August U5 August) kJ, + ** one one one one ----- B7 V. Description of the invention (speaking) 6 4,55 〇HUMS: 519.0958 〇TLC (silicone, GF): Rf = 0.23 40% ethyl acetate / hexane. Example 302 4,5-Dioxocyclopropyl (5,6,7,8,9,10-Hexa-4-anyl-2-oxy-2H-cyclooctyl [b] e diran: _3_ (Methyl) methyl] phenyl] -2-thiophenamidamine physical properties are as follows: White amorphous solid MS (FAB): 554, 338, 217, 207, 144 · in, 55, 400 HRMS: 554.0627 ° TLC (silicone GF): Rr = 0 '26 4σ% · ethyl acetate / hexane. Example 30 3 4,5-Dibromo-N- [3- [Cyclopropyl (5,6,7,8,9,10-Hexazone-4 -Ethyl-2-oxy-2'-cyclooctyl [ b] B-Zanan-3-yl) methyl] phenyl] -2-thiapansulfonamide The physical properties are as follows: White amorphous solid HS (FAB): 644,642, 338, 247, 217, 207, 195 , 144,55. HRHS: 641.9627 ° TLC (silicone GF): Rf = 0.23 40% ethyl acetate / hexane. Example 304 2,5 -Dichloro-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Slightly ran-3-yl) methyl] phenyl] -3-thiophenesulfonamide r- The physical properties are as follows: -260- This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) ---- --- I-- 装-(Please read the note on the back τ ^ before filling this page)

ST Line Patent No. 83100644 Patent Application Revised Chinese Manual (August 85) kT B7 V. Description of the Invention () White Amorphous Solid MS (FAB): 554, 338, 207, 144, 69, 55. HRMS: 554.0621 〇TLC (silicone GF): Rf = 0.21 40% ethyl acetate / 3 Example 305 2,4-difluoro-1 [3- [cyclopropyl (5,67. * * * 0, -4- [Hydroxy-2-oxy-2H-cyclooctyl]] Phenylbenzsulfenamine physical properties are as follows: White amorphous solid MS (EI): 547, 520 91 〇HRMS: 547.0983 ° TLC (sand Gum 'GF): Rf = 0.28, 40% ethyl acetate / hexane. Example 306 2,4,6-trioxane]-[3- [Cyclopropyl (5,6,7,8,9,1〇 -Hexahydro-4-Cytyl-2-oxy-2H-cyclooctyl [b] yells "3-yl) methane. 9,10-hexakis 3 ~ yl> methyl news 207, 144, 13 〇, ii7. F Please read the notes on the back Jr-s: 'iA-k • this page)... &Quot; phenyl] phenyl] -benzsulfonamide physical properties are as follows: white amorphous solid': HS (EI): 581, 555, 338, 310, 270, 233, 207, 180, 144 ° HRMS: 581.6597 〇TLC (silicone, GF): Rf = 0, 28, 40% ethyl acetate / hexane. Examples 30 7 N- [4-[[3- [Cyclopropyl (5, 6,7, 8,9, 10-hexahydro-4-controll ~ yl-2-oxy-2H-cyclooctyl [b ] Piperan-3-yl) methyl] benzyl ~ 261-This paper size applies to China National Standard (CNS) A4 specification (210X297 mm)-line · Printed A7. 'B7 Patent Application No. 83100644 by the Consumer Standards Cooperative of the Ministry of Economic Affairs of the People's Republic of China (August 85. Description of the invention _] Amine] Sulfonyl] Phenyl] Acetamide As follows:. White amorphous solid MS (EI): 536, 507, 465, 338, 233, 207, 186, 156, 144, 50. HRMS: 5 36. 19 9.3 ° TLC (silicone, GF): Rf = 0.25 4% methanol / dichloromethane. Example 308 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-.4-hydroxy- 2-oxy-2H-cyclooctyl [ b] piperan-3-yl) methyl] phenyl] 4- (benzylazo) -benzylamine The physical properties are as follows:-Orange amorphous solid MS (EI): 583, 338, 233, 186 , 144, 105, 77 HRMS: 583.2133 ° TLC (silicone GP): Rr = 0.62 4% methanol / dichloroethane. Example 309 1 «-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxyj 2-oxy-2H-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl] 4-[[4- (dimethylkyl) phenyl] azo] -benzenesulfonium p-u-103389 The physical properties are as follows: Red amorphous solid HS (FAB): 627 , 224 HRMS: 627.2660 ° TLC (silicone, GF) ·· Rf -262 This paper size is applicable to China National Standard (CNS) Α4 specification (210 × 297 mm) —. Pack. Order], 矣. 、 二 (Please read the back first Please pay attention to this page and then fill in this page) Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs &quot;. 148, 135, 120 ° 0.60 4% methanol / dichloromethane. 83100 & 44 Patent Application Revised Chinese Manual Revised Page U5 Aug. 5) A7 --------------------- ---------- -· · B7 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention Ut \) Example 310 N- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4 -Hydroxy- 2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (2-pyridyl) -2-thiophenesulfonamide The physical properties are as follows: Crystalline solid MS (EI): 562, 533, 367, 338, 304. 194, 176. 16Ϊ, 144, 116, 55 〇HRHS: 562.1295 〇TLC (silicone GF): Rr = 0.37 20% Z / ethyl acetate / Dimethane. Example 311 3-Ano-N- [3- [cyclopropyl (5,6, 7,3,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -2-methyl-benzenesulfonamide. Physical properties are as follows: White amorphous solid MS (EI): 527, 49 9, 338, 310, 274, 233, 207, 144, 125. 91, 79. HRHS: 327.1527 ° TLC (silicone GF): R / = 0.2Ϊ 40% ethyl acetate / hexane. Example 3 2 Ν- [3- [cyclopropyl (5,6,7,8,9. 10-hexahydro-4-hydroxy- 2-oxy-2-cyclooctyl [b] piperan-3-yl) The physical properties of methyl] phenyl] -4- (trifluoromethoxy) benzenesulfonamide are as follows: _ White amorphous solids MS (EI): 563, 535, 338, 309, 233, 207, 144. -263- This paper size is in accordance with Chinese National Standard (CNS) A4 (2 丨 OX297mm) (Please read the precautions on the back before writing this page.) Cooperative printed No. 83 100644 of Chinese patent application amendment page U5 August 2015 A7 B7 V. Description of invention (HRMS: 563.1596 «TLC (silicone GF): Rr = 0.33 40% ethyl acetate / hexane. Example 313 3-chloro-N- [3- [cyclopropyl (5,6 · 7,3 · 9,10-hexahydro-4-hydroxy-yl-2-oxy-2Η-cyclooctyl [b ] Piperan-3-yl) methyl] phenyl] -3-[(benzenesulfonyl) amino] -1-propanesulfonamide (Formula Z-3, where Rei is 3-U-propanesulfonium Amine) phenyl) See z-graph. A solution of the title product 353 (100 mg), chloropropylsulfonyl chloride (40 mg) and pyridine (50 µl) in dichloromethane (4 ml) was stirred at room temperature for 18 hours. The crude reaction mixture was chromatographed on silica gel to give the title compound (75 mg) as a colorless glass. The physical properties are as follows: ._ White amorphous solid MS (EI): 634, 534, 505, 494, 338, 309, 233, 207, 144 〇HRMS: 6 35.1655 〇TLC (silicone GF): Rr = 0.60 50% acetic acid Ethyl ester / dichloromethane. Preparation 55 3-pyridinesulfonate To 1.2 g of 3-pyridinesulfonic acid (Aldrich Chemical Co.) was added 1.70 g of PCU and 5.4 ml of POCU. The reaction mixture was heated to reflux temperature and allowed to stir under reflux for 5 hours. The reaction mixture was cooled to room temperature and evaporated (under vacuum) to dryness. The solid residue was partitioned between dichloromethane and a saturated aqueous solution of sodium bicarbonate, and the organic phase K aqueous solution of sodium bicarbonate was washed twice, and then dried over anhydrous sodium sulfate. 'Yes, the organic solution is evaporated to dryness to produce 900 ·-·. Mg of the title compound, which can be directly used in the preparation of sulfonamide. The physical properties are as follows: Colorless oil. -2 6 4-This paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) II. Approval for clothes order I ^ line ......., j. ') (Please read the notes on the back &quot; Fill in [Malay Page] Revised page of Chinese Specification for Patent Application No. 83100644 printed by the Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (August 1985) 5 8.9.9-8.92, 8.35-8.31, 7.64- 7.59 ppm ° Preparation 56 5-methyl-3-pyridinesulfonyl chloride is prepared in a similar manner to 55, but replaces 5-methyl-3-pyridinesulfonic acid (SUma -Aldric.h) to prepare the title product. Physical properties are as follows: White crystalline solid. 1 Η NMR (CDC 1 3) 3 7.8 5-7. 8 3, 7. 5 6-7.4 7 ppa. Example 314 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b]: piperan-3-yl) methyl] Phenyl]-3-pyridinesulfonamide—_ The method of Example 264 was used, but the title compound was prepared using the above titled sulfonaminium chloride of Preparation 55. Physical properties are as follows: White amorphous solid. HRMS: 480.1725 ° MS ( EI): 480, 45 1, 338, 274, 248, 233, 207, 1 44, 130, 117, 106, 79, 67, 55, 41 ° TLC (silicone GF): Rr = 0.8 (ethyl acetate). Example 315 H- [3- [cyclopropyl (5,6, 7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclohexyl [^)] piperan-3-yl) methyl] phenyl] -5-methyl-3_pyridine Sulfonamide was prepared by the method of Example 264, but using the title sulfonium chloride of Preparation 56, to make the title compound. Wide physical properties are as follows: _ White amorphous solid. HRHS: 494.1878 ° -265- _ This paper size is applicable to Chinese National Standard (CNS) A4 size (210X29 * 7mm) (Please read the precautions on the back before filling this page) -pack-

, 1T line Ministry of Economic Affairs, Central Standards Bureau, Employees' Cooperatives, printed No. 83100644, Patent Application Inspection, Chinese Manual, Revised Page (August 1985) A7 ^ B7 V. Description of Invention ρθ) MS (EI): 494, 465, 453, 338 , 301, 288, 262, 233, 207, 186, 144, 130, 92 ° TLC (Silicon, GF): Rf = 0.8 (ethyl acetate). Examples 316-347 Other methods of the present invention can be prepared using methods similar to those of Example 264 and using a commercially available suitable sulfonium. Example 316 N- [3- [cyclopropyl (5, 6.7, 8,9, 10-hexahydrohydroxy-2-oxy-2H-cyclooctyl [b] piperan.-3-yl) methyl] benzene Glycol ethylenesulfonamide ^. Physical properties are as follows: --- White amorphous solid. HRMS: 429 · 1617. TLC. (Silicone, GF): Rf = 0.4 (5% formazan / chloroform). Example 317 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] '^ diran_3- (Methyl) methyl] benzyl] -methanesulfonamide physical properties are as follows: White amorphous solid bet. ... HRMS: 417.1619 〇 TLC (Sand _ 'GF): Rf = 0.4 (5% methanol / aerosol). Example 318 fluorene- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-fluorenylhydroxy-2 -oxy-2'-cyclooctyl [b] thioan_3-yl) formyl Base] benzyl] •• Ethylsulfonamide f The physical properties are as follows: -266- This paper size applies to China National Standard (CNS) A4 specification (210X297 male sauce) (Read the note on the back first, and then fill in this page )-Binding and Binding No. 83 100644 Patent Application Chinese Specification Revised Page (August 1985) A7--B7 V. Description of the Invention (White Amorphous Solid. HRHS: 431.1760 ° TLC (Silicone, GF): Rf = 0.3 (5% methanol / chloroform). Example 319 H- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [ b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide physical properties are as follows: white amorphous solid. HRHS: 679.1750 〇TLC (silicone GF): Rr = 0.4 (5 ^ methanol / chloroform). Example 320 N- [3- [Cyclopropyl (5,677,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzene The physical properties of phenyl] -2-phenyl-ethylenesulfonamide are as follows: White amorphous solid. HRMS: 505.1933 ° TLC (silicone GF): iU = 0.4 (5% methanol / chloroform). Example 321 H- [3- [cyclopropyl ('5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl] -benzylmethanesulfonamide physical properties are as follows: white amorphous solid. _-HRMS: 493.1922 ° ^ TLC (silicone GF): Rf = 0.3 (5% methanol / atmosphere). -267- This paper size applies to China National Standard (CNS) A4 (210X 297mm) binding. ~ 矣 (Please read the note on the back #Cuck and fill out this page) Printed by the Central Standards Bureau of the Ministry of Economic Affairs and Consumer Cooperatives Standard Bureau employee consumer cooperative printed patent application No. 83100644 A7-revised Chinese manual (August 85) B7 V. Description of the invention (Example 322 ^ 1- [5-(: [[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorene The physical properties of the methyl] -4-methyl-2-thiazolyl] -acetamide are as follows: White amorphous solid. HRHS: 557.1652. TLC (silicone GF): Rr = 0.15 (5% methanol / chloroform). Example 323 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] -piperan-3-yl ) The physical properties of methyl] phenyl] -2-thiophenesulfonamide are as follows: — \ White amorphous solid. HRHS: 485.1323 ° TLC (silicone GF): Rf = 0.2 (5% methanol / chloroform). Example 324 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] pyran-3-yl) The physical properties of methyl] benzyl] -sulfenamide are as follows: '...' · White amorphous solid. HRMS: 445.1928 ° TLC (silicone GF): Rf = 0.3 (5% methanol / chloroform). Example 325 N- [3- [Cyclopropyl (_5, δ, -7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctane [bί ^ t ^ 农 兰 -3 -Methyl) methyl] phenyl]-. 4-methyl-benzenesulfonamide-268- This paper size is applicable to the Chinese National Standard (CMS) A4 (210X297 mm) I --------- Binding system (Tian Min Min reads the note on the back of the arm 'refill t page) No. 8310064 No. 4 Patent Application A7 Chinese Manual Correction Page (85 months δ) = Β7 V. Description of the invention The physical characteristics are as follows: White amorphous solid. HRHS: 493 · 1932 〇 TLC (silicone GF): I = 0.4 (5% methanol / chloroform). Example 326 hydrazone- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan: -3-yl ) Methyl] phenyl]-1-Butanesulfanilamine has the following physical properties: __ Amorphous white solid. HRMS: 459.2087 〇 TLC (silicone GF): 1 = 0.4 (5% methanol / chloroform). Example 327 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl) The physical properties of methyl] phenyl] -1,3-dihydro-1,3-dioxy-2H-isoindole-2-ethanesulfonamide are as follows: White amorphous solid. HRMS: 576.1923 ° ‘TLC (silicone GF): Rr = 0.4 (5% methanol / chloroform). Printed by the Employees' Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the matter on the back: fill in this page first) Example 328 N- [3- [cyclopropyl Hydrogen-4-hydroxy- 2-oxy-2H-cyclooctyl [b-] piperan-3-yl) methyl] phenyl] -2-propanesulfonamide_ "Physical properties are as follows: White amorphous solid. -269- Printed Chinese Manual for Patent Application No. 83100644 of the Central Standards Bureau of the Ministry of Economic Affairs, Amendment Sheet of Chinese Specification (August 85) $ 5. Description of Invention (&gt;#) HRHS: 445.1928 ° TLC (Silicone GF): Rf = 0.3 (5% methanol / chloroform). Example 329 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctane [b] piperan-3-yl) methyl] phenyl] -2, 6-dimethyl-benzenesulfonamide The physical properties are as follows: White amorphous solid. HRMS: 507.2082 ° TL C (silicone, GF): R f = 0.5 (50% ethyl acetate / hexane). Example 330 N- [3- [Cyclopropyl (L6,7,8,9,10-hexahydro.-4-hydroxy-2- 2- The physical properties of oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-methyl-benzenesulfonamide are as follows: White amorphous solid. HRMS: 493.1929 ° TLC (silicone, GF ): 0.5 (50% ethyl acetate / hexane). Example 331 3-chloro-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2) -Oxy-2fT-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-propanesulfonamide The physical properties are as follows: White amorphous solid. HRMS: 679.1544. _ TLC (Silicone GF) : = 0.5 (&amp; Ό% ethyl acetate / hexane). Example 332 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- -270- This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the note on the back before filling in this page). Packing. Application Δ7 &quot; Correction Sheet of Chinese Manual (August 85) B7 V. Description of the Invention 2-oxy-2Η-cyclooctyl [b] pyran-3-yl) methyl] phenyl]-3.5-bis ( The physical properties of trifluoromethyl) sulfenamide are as follows: White amorphous p-body. HRHS: 616.1631 ° TLC (silicone GF): Rr = 0.5 (50% ethyl acetate / hexane + 0.5% acetic acid).洌 333 N-C3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b / l · 叫 嘀 -3- Group) methyl] phenyl] -7,7-dimethyl-2-oxo j-bicyclo [2.2.1] heptane-: l-methanesulfonamide physical properties are as follows: White amorphous solid. HRHS: 553.2507 TLC (silicone, GF): Rf = 0.5 (50% ethyl acetate / hexane). Example 334 H- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] v ^ 底 RAN_3- Group) methyl] phenyl] _ 2.6-dimethoxy-dosulfenylamine Physical properties are as follows: White amorphous solid. HRHS: 539.1983 ° TLC (silicone GF): Rr = 0.5_ (50% ethyl acetate / hexane). Example 335 N- [3- [Cyclopropyl (5, t, 7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl-3-byl) Methyl] phenyl]--271- This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the note on the back before filling this page).

, ST-line Ministry of Economic Affairs, Central Standards Bureau, Consumer Consumption Cooperatives, printed the Chinese specification for Patent Application No. 83100644 (August 85) A7 B7 V. Description of the invention (&gt; 7, 3, 4-dimethoxy-benzene The physical properties of sulfonamide are as follows: White amorphous solid. HRHS: 539.198 1 〇TLC (silicone GF): Rr = 0.5 (50% ethyl acetate / hexane). Example 336 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3-methyl -Sulfametamine has the following physical properties: 彳: White amorphous solid. 1: HRMS: 493.1931 〇TLC (silicone GF): Rf = 0.5 (50% ethyl acetate / hexane). Example 337 2-Bromo-N -[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] The physical properties of phenyl] -6-methoxy-benzenesulfonamide are as follows: White amorphous solid. HRMS: 588.1060 ° TLC (silicone GF): Rr = 0.4 (50% ethyl acetate / hexane). Example 338 » -[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Phenyl] -3,5-dimethyl-47 isozazolium The physical properties are as follows: ^ White amorphous solid. (Please read the notes on the back before filling this page). Binding · Thread-272- This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) Article 83100644 Revised Page of Chinese Specification for Patent Application No. (August 1985) A7 'B7 V. Description of Invention (βι) HRMS printed by Employee Consumer Cooperatives of Central Bureau of Standards of the Ministry of Economic Affairs: 498.1822 〇TLC (Silicone GF): Rf = 0.4 ( 50% ethyl acetate / hexane). Example 339 2-cyano-N- [3- [cyclopropyl (5,6.7,8,9,10-hexahydro- 4-hydroxy-2-oxy-2H -Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide The physical properties are as follows: White amorphous solid. HRMS: 504.1713 〇TLC (silicone GF): Rf = 0.4 (50 % Ethyl acetate / hexane). Example 340 N- [3- [Cyclopropyl (5, J, _7,8,9,10-Hexa-4-Hydroxy-2-Hydroxy-2H-cyclooctyl [ b] piperan-3-yl) methyl] phenyl] -2,1,3-benzothiadiazole-4-sulfonamide The physical properties are as follows: White amorphous solid. HRMS: 537.1391 ° TLC (silicone, GF): = 0.4 (50% ethyl acetate / hexane). Example 341 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclo 4 '[b.] Piran-3- (Methyl) methyl] phenyl]-.; 4-Ethyl-benzenesulfonamide has the following physical properties: White amorphous solid. HRMS: 507.2083 ° __ TLC (silicone, GF): Rf = 0.4 (* 50% ethyl acetate / hexane). Example 342 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 273-)-This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) (Please read the note on the back before filling out this page)-Assembling and ordering printed by the Consumer Standards of the Central Standards Bureau, Ministry of Economic Affairs, No. 83100644 Patent Application ~ A7 Chinese Manual Correction Page (August 85) Description of the invention (2-oxy-2H-cyclooctyl [b] 17 diamino-3-yl) methyl] phenyl] 4-propyl-benzenesulfonamide The physical properties are as follows: White amorphous body. HRMS : 521.2241 ° TLC (silicone, GF): Rf = 0.4 (50% ethyl acetate / hexane). Example 343 [3- [cyclopropyl (5,6,7,8,9,10-hexahydro- The physical properties of 4-hydroxy- 2-oxy-211-cyclooctyl [1 &gt;] piperan-3-yl) methyl] phenyl] -1-octanesulfonamide are as follows: One, two 'white amorphous solid HRMS: 516 · 2767 ° TLC (silicone, GF): Rf = 0.4 (50% ethyl acetate / hexane) ° Example 344 H- [3- [cyclopropyl_ (5,6,7,8,9, The physical properties of 10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] I ^ diran_3-yl) methyl] phenyl] _ dodecanesulfonamide are as follows: Crystalline solid '': HRMS: 571.3327 ° TLC (silicone GF): Rf = 0.4 (50% ethyl acetate / hexane). Example 345 H- [3- [cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-r ~ 4- U-methylethyl) -benzenesulfonamide The physical characteristics are as follows: (Please read the note on the back & fill in this page first). Binding line -274- This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) A6 B6 Central Standard of the Ministry of Economic Affairs Printed by the Bureau's Consumer Cooperatives V. Invention Description (273) White amorphous solid. HRMS: 521.2228 ° TLC (silicone GF): Rf = 0.4 (50% ethyl acetate / hexane). Example 346 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] pyran-3-yl) The physical characteristics of methyl] benzyl] -phenylethanesulfonamide are as follows: White amorphous solid. HRMS: 507.2086. TLC (silicone GF): Rf = 0.4 (50% ethyl acetate / hexane). Example 347 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] lttane-3-yl) The physical properties of methyl] benzyl] -5- (3-isooxazolyl) -2-thiophenesulfonamide are as follows: White amorphous solid. HRMS: 552.1390 ° TLC (silicone GF): Rf = 0.4 (50% ethyl acetate / hexane). Example 348 4-Amino-N- [3- [cyclopropyl (5,6,7,8,9,; 10-hexamidine-4-hydroxy-2-oxy-2H-cyclooctyl [b] py Nan-3-yl) methyl] phenyl] -benzimidazine and N- [3- [cyclopropyl (5, 6,7,8,9, 10-hexahydro-4-meryl-2- Oxy-2H-cyclooctyl [b] l% an-3-yl) methyl] phenyl] -4- (hydroxylamino) benzenesulfonamide (formula Z-3, where Re aminophenyl or 4- (Hydroxylamino-phenyl) See Z-graph. (Please read the notes on the back before filling this page)

. 、 TT _dream-

-275- This paper size applies to Chinese National Standard (CNS) f 4 specifications (210 X 297 mm I printed by A6 B6, Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs) 5. Description of the invention (.2 * 74) Example 273 Title Compound U65 Mg) and a mixture of 10% Pd / C (50 mg) in ethyl acetate (30 ml), hydrogenated by shaking at 20 psi for 2 hours, filtered through a plug, and washed with ethyl acetate. The filtrate was concentrated in vacuo and chromatographed on silica gel to produce 140 mg of the first title compound and 260 mg of the second title compound as a white amorphous solid. The physical properties of the first title compound are as follows: MS (EI): 694, 338, 310, 212, 186, 156, 144, 132, 108, 92 ° HR MS: 494.1876 ° TLC (silicone, GF): Rf = 0.26 3 % Methanol / dichloromethane. The physical properties of the second title compound are as follows: HS (FAB): 511, 495, 338, 247, 207, 195. TLC (silicone * GF): Rf = 0.1 (3 3% methanol / dichloromethane. Example 349 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxyl -2-oxy-2H-cyclooctyl [b] pyran-3-yl) methyl] phenyl] -4-[(phenylsulfonyl) amino] -benzylsulfonamide (Formula Z-3 * Where Rel is 4 [(phenylsulfonyl) amino] phenyl) see Figure Z. Example 348 First title compound (28 mg), benzylsulfonyl chloride (10 μl), and pyridine (14 μl Liter) in dichloromethane (2 ml) and stirred at room temperature for 18 hours. The crude product was chromatographed on silica gel to produce 1 δ mg of the title compound as a white amorphous solid. The physical properties are as follows: MS (ΕΙ): 634, 477, 442, 339, 310, 265, 233, 194, 144, 124, 77 ° -276- This paper size applies to Chinese national standards (CNS 丨 A4 specification (21〇X297)) &quot; &quot; {Please read the precautions on the back before filling this page). Install A6 B6 Printed by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (275) HRHS: 634.1822 ° TLC (silicone GF): Rf = 0.21 40% acetic acid Ethyl ester / hexane. Example 350 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4- -2-oxy-2H-cyclooctyl [b] pyran-3-yl) methyl] phenyl]-3-[(benzylsulfonyl) amino] -benzylsulfonamide (Formula Z- 3, where R81 is 3-[(phenylsulfonyl) amino] phenyl) see Figure Z. Using the same method as in Example 349, starting from the first title compound of Example 353, the title compound can be obtained. Physical properties As follows: White amorphous solid. MS (EI): 634, 605, 493, 338, 233, 207, 1 44, 77 ° HRMS: 634.1811 ° TLC (silicone, GF): = 0,11 40% ethyl acetate / Hexane. Example 351 1 ^-[3-[[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [ b] pyran-3-yl) methyl] benzyl] amino] sulfofluorenyl.phenyl] phenylbenzylamine (formula Z-3, where Rei is 3- (benzylfluorenyl) phenyl) see Figure Z. Using the same procedure as in Example 349 above, and using the first title compound and benzamidine chloride from Example 353, the title compound can be obtained from a white amorphous solid. The physical properties are as follows: MS (EI): 598, 493, 338, 212, 186, 144, 1 32, 105 ° HRMS: 598.2133 ° (Please read the precautions on the back before filling this page) Binding-binding-weft.

J -277-Zhang Chi / Li Shi-Use Chinese National Standard (CNS) T4 (210x297 mm) Patent Application No. 83100644 printed by Bei Gong Consumer Cooperatives, Central Standards Bureau of the Ministry of Economic Affairs. August) B7 —— 1-_ ____________________________ V. Description of the invention (37 () TLC (silicone · GF): Rf = 0.11 40% ethyl acetate / hexane. Example 352 N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-. (Dimethylamino) -benzenesulfonamide (Formula Z-3m where Ral is 4-dimethylaminophenyl) See Figure Z. The first title compound of Example 348 (50 mg) in methanol (3 ml) The solution was treated with K-formaldehyde (24 g), refluxed for 45 minutes, and cooled to room temperature. Then treated with K cyanoborohydride (20 mg), and then stirred at room temperature for 18 hours. Mixture M water Discontinued, diluted with ethyl acetate, washed the organic layer with water, brine, and dried (anhydrous sodium sulfate, filtered, and reduced to chromatography on silica gel to produce 35 mg of the title compound. Physical properties are as follows: White amorphous Solid MS (E1): 522, 338, 184, 136, 120. HRHS: 522.21 90 0 TLC (silicone, GF): Rf = 0.41 50% methanol / dichloromethane. Example 353 3-amino-N- [3- [ Cyclopropyl (5,6,7,8,9,10-hexahydro-4_hydroxy_2_oxy'_2H, _cyclooctyl j; b] piperan_3_yl) methyl] ... Phenyl] -benzenesulfonamide and N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) methyl] phenyl] -3- (hydroxylamino) -benzenesulfonamide (Formula Z-3, where Ral is 3_-amine * phenyl or 4-hydroxy-aminobenzyl) See Figure Z. Example 274 title compound (600 mg) and 10% Pd / C (100 mg) at -278- This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the back Note: ΚΛ refill this page ¾)-Binding and Binding Printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Printed No. 831 00644 Patent Application Chinese Chromium Page (Aug'85 &gt; A7 'B7 5 2. Description of the invention U77) A mixture of ethyl acetate (.30 ml), hydrogenated by shaking at 20 psi for 2 hours, then passed through a plug, and washed with ethyl acetate. The combined filtrate was concentrated in vacuo and Chromatography on silica, 380 mg of generating a first title product and 260 mg of the second title product as a white amorphous crystalline solid Tui particles. The physical properties of the first title product are as follows: White amorphous solid. MS (EI): 494, 466, 338, 309, 233, 207, 186, 144, 92. Two ... HRMS: 494.1885 ° TLC (silicone GF): Rf = 0.28 5% ^ alcohol / dichloromethane. The physical properties of the second problem product are as follows: · White amorphous solid. MS (EI): 510, 495, 371, 340, 247, 207, 144, 118. HRMS: 511.1905 TLC (silicone GF): .1 = 0.23 5% methanol / dichloromethane. Example 354 3-[[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- Methyl) phenyl] phenyl] amino] sulfofluorenyl] benzoic acid, methyl ester (Formula Z-3, where Rei is 4-methylbenzoate) See Figure Z. The title compound of Example 292 ( 300 mg) and concentrated sulfuric acid (300 microliters) in methanol (10 ml) at room temperature for 2 days, diluted with ethyl acetate, washed with water, brine, dried (anhydrous terpene acid), filtered , Concentrated and chromatographed on silica gel to produce 22 5 mg of the title compound. The physical properties are as follows: ------ 2.7-Q-This paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) --- -----.-- Approve clothes ------- ΙΤ ---- (Please read the cautions on the back to fill out this education). No. 83100644 Patent Application Revised Chinese Manual Correction Page ( August 8) Α7 Β7 V. Description of the invention P7 |) Printed white amorphous solid by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs. MS (EI): 537, 509, 476, 338, 233, 207, 185, 144 ° HRMS: 537.821 〇TLC (silicone GF): Rf = 0.38, 40% ethyl acetate / hexane. 355 N- [g- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl Phenyl] -phenyl]-3-[(2-ethyl9) amino] benzidine and H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro "-4 , Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl "^ yl] -3-[(bis- (2-ethanol)) amino] -benzenesulfonamide ( Formula &quot; Z: 3, where ^ 1 is 3-[(2-ethanol) amino] phenyl or 3-[(bis- (2-ethanol) amino] phenyl) See Figure Z. Example 353 first A solution of the title compound (50 mg) and para-toluenesulfonic acid (5 mg) in methanol (2 ml) was cooled to -70¾ in a flask equipped with a dry ice condenser. Ethylene oxide (5 ml) was condensed to In the solution, the solution was stirred at ambient temperature for 18 hours, and then concentrated in vacuo. The crude product was chromatographed on silica gel to produce 30 mg of the first title product as a white amorphous solid and 10 mg of the second title product as white. Amorphous solid. The physical properties of the first title product are as follows: MS (EI): 538, 520, 507, 491, 368, 338, 233, 186, 144, 1050- HRMS ·· 538.2126 ° Wide TLC (Silicone GF) : Rf = 0.30 50% acetic acid Ester / dichloromethane. The physical properties of the second title product are as follows: -9 Λ 0-(Please read the precautions on the back #Fill this page first). Installation-,-· β The size of this paper applies the Chinese National Standard (CNS) Α4 specification (210 × 297 (Mm) Patent Application No. 83100644, Chinese Revised Sheet of Chinese Specification (August 1985) A7 ~ _ B7 V. Description of Invention (MS (EI): 582, 564, 551, 521, 505, 357, 338, 214, 144 , 105. HRMS: 582.2446 o TLC (silicone GF): Rf = Oh 50% ethyl acetate / dichloromethane. Example 356 [3- [Cyclopropyl (5,6,7,8,9,10- Hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3_ [methanol] -benzenesulfonamide (Formula Z-3, where Rei (It is 3-methanol-phenyl). See Figure Z. Example 354 title product (50 mg) color _ 0 = 0 solution in anhydrous tetrahydrofuran 'K lithium aluminum hydride treatment (5 mg). Carriers under 0¾ Stir for 30 minutes, stop in Μ water, dilute with ethyl acetate, wash with hydrochloric acid, water, and brine, dry (anhydrous sodium sulfate), purify, and concentrate under vacuum * and chromatography on silica gel can produce 45 mg of the title compound, White solid The physical properties are as follows: MS (EI): 509, 491, 481, 463, 388, 233, 220, 207, 186, 144 ° HRMS: 509 · 1883. TLC (silicone GF): Rf = 0.27 40% ethyl acetate / Hexane. Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. Example 357 N- [3- [Cyclopropyl (5,6,7,8,9,10 -Hexahydro-4 -hydroxy-2-oxy- 2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- (2-isothiapyridinyl) benzenesulfonamide-s, S'-dioxide (formula Z-3 · Among them is X2-isothiazolyl) phenyl) see Z diagram. Title product of Example 363 (25 mg), sodium iodide (7 mg), and morphine _- 281 -_ This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) Employees of the Central Standards Bureau of the Ministry of Economic Affairs Consumption Cooperative printed the Chinese Specification for Patent Application No. 83100644 (August 85) A7 _______B7 V. Description of the invention (&gt; f) A solution of morpholine (17 μl) in acetonitrile (2 ml) was heated under reflux for 24 hours, Cooling, diluting with ethyl acetate, K water, washing with brine, drying (anhydrous sodium sulfate), filtering, concentrating in vacuo and chromatography on silica gel yielded 15 mg of the title product. The physical properties are as follows: White amorphous solid. MS (EI): 598, 569, 534, 505, 338, 309, 233, 207, 186, 1 44... TLC (silicone GF): Rf = 0.40, 50 ethyl acetate / dichloromethane. Example 358-362 Other compounds of the present invention can also be prepared by following the steps of the above example: see Figure Z. Example 358 H- [3- [cyclopropyl (5, δ, 7, δ, 9,10-hexahydro-4) -Hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-3- (2-methoxyethoxymethoxy) -benzenesulfonate 359 M- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl Phenyl] phenyl] -3-hydroxy-benzenesulfonamide Examples of 360 N- [3- [cyclopropyl (5,6,7,8,9,: 10-hexahydro-4-hydroxy- 2-oxy -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-3- (4-morpholine ethoxy)-benzenesulfonamide example 361 H- [3- [cyclo Propyl (5,6,7rT8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-3- (H , H-Diethylaminoethoxy) benzenesulfonamide_; _- 282 -__ This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) --------- equipment ------ Order ------ line ..) /-.. (Please read the note on the back V 苒 Fill this page first) Printed Patent No. 83100644 by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Application for amendment of Chinese manual U5 August) Q5. Description of the invention (y) Example 362 H- [3- [Cyclopropyl (5,6,7,8,9,: 10-hexahydro-4-Cyclo-2-oxyl -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] _ 4-hydroxy-benzenesulfonamide to prepare 57 aminocarboxylic acids, [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclohepta [b] piperan-3-yl) methyl] phenyl]-, phenylmethyl ester, see CC diagram . To 17.5 mg of para-toluenesulfonic acid was added toluene (50 ml), which was heated to reflux (under a nitrogen atmosphere) * and 10 ml of toluene was azeotroped from the autoreactive solution. The mixture was cooled to 20 scoops, and then 2 mg of 2H-cyclooctane [b] -2-an and 1.065 g were added to prepare 52 standard amidine products. The reaction allowed it to search for 72 hours at 20¾. The reaction mixture was poured into 100 ml of ethyl acetate, and the ethyl acetate solution K was saturated with a sodium bicarbonate aqueous solution and a saturated sodium chloride aqueous solution, and dried over anhydrous sodium sulfate. The organic solution was evaporated to dryness to give 1.48 g of the crude title compound. Chromatography on silica gel with 50% ethyl acetate / hexane (with 0.5% acetic acid) gave 1.13 g of the pure title product as a colorless solid. The physical properties are as follows: White amorphous solid. HRMS: 459.2041 ° MS (EI): 459, 431, 415, 368, 350, 340, 324, 280, 230, 219, 186, 158, 144, 91, -55 ° 1 ^ (: (Silicone, Factory 0) : 1 ^ = 0.75 (5X methanol / aqueous imitation).

Rr = 0.80 (50% ethyl acetate / hexane plus 0.5% acetic acid) Preparation of hydrazone 58 3-[(3-aminophenyl) cyclopropylmethyl] -5,6,7,8,9,10 -六 ______- 283-__ This paper size applies to China National Standard (CNS) A4 (210X 297 mm) ---------- Approval of clothes ------, order ---- Ts— · ^; a) &gt; i {(Please read the note on the back &gt; &lt; fill in this page well) The Central Consumers Bureau of the Ministry of Economic Affairs printed the Chinese explanation of the patent application No. 83 100644 of the Central Government Bureau 蓍 amendment Page (August 1985) A7 ~ B7 V. Description of the invention (Mhydro-4-hydroxy-2Η-cycloheptan [b] piperan-2-one, see CC picture. To 970 mg of 57 title product, add 100 ml of human methanol and 240 mg of 10% pd / C. The reaction mixture was primordiated under 48 pounds of hydrogen for 18 hours. The reaction mixture was triturated, washed thoroughly with ethyl acetate and evaporated to dryness to yield 6 32 mg of the crude title compound. The crude product was dissolved in 5 ml of dichloromethane, 'passed through a plug and evaporated to dryness,' which produced 560 mg of the title product as an amorphous solid. /. Physical properties are as follows: White amorphous solid. 4 — HRMS: 325 1675 ° MS (EI): 325, 30 8, 296, 282, 240, 213, 187, 172, 159, 146, 130, 1 17, 106, 91, 55. UC (silicone, GF): Rf = 0.4 (5% methanol / chloroform). I = 0_3 (33% Acetone / Cyclohexane). Examples 363-365 Using similar procedures as above and suitable sulfonium chloride, and preparing the title product of 58 instead of the title product of preparation 57, other compounds of the present invention can be prepared: see CC diagram Example 363 N- [3- [Cyclopropyl (2,5,6,7,8,9-hexahydro-4-hydroxy-2-oxycyclohepta [b] piperan-3-yl) methyl ] Phenyl] •• Ethylsulfonamide has the following physical properties: White, non-crystalline solid. ________ ~ 2 8 4--_ I — This paper size applies to China National Standard (CNS) A4 (210X297 mm) I- ------- batch clothes ------, 1T ----- line..I. I .. one (please read the note on the back # before filling-this page), 'Ministry of Economy Printed Chinese Version of Patent Application No. 83100644 by the Consumer Standards of the Central Standards Bureau Amendment Page (August 1985) V. Description of Invention (/ ¾ HRMS: 325.1675 〇MS (EI): 325, 308, 296, 282, 240 , 213, 187, 172, 159, 46, 130, 117, 106, 91, 55. TLC (silicone GF): Rf = 0.3 (33% acetone / cyclohexane Example 364 H- [3- [cyclopropyl (2,5,6,7,8,9-hexahydro-4-hydroxy- The physical properties of 2-oxycyclohepta [b] piperan-3-yl) methyl] phenyl] -methanesulfonamide are as follows:…… white amorphous solid. __ HRMS: 403.1463 °… MS (EI): 403 , 375, 362, 324, 295, 265, 233, 219, 193, 158, 144, 130, 117, 91, 79 ° TLC (silicone GF): Rf = 0.3 (33% acetone / cyclohexane). 365 H- [3- [cyclopropyl (2,5,6,7,8,9-hexahydro-4-hydroxy-2-oxycycloheptyl [b] piperan-3-yl) methyl] benzene The physical properties of the group] -ethanesulfonamide are as follows: White amorphous solid. HR MS: 417.1607 〇MS (El): 417, 389, 376, 324, 306, 295, 279, 219, 193, 158, 144, 130 , 117, 91,-55. TLC (silicone GF): Rf = 0.3 (33% ^ acetone / cyclohexane). Example 365A 4-[[[3- [cyclopropyl (5,6,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amine: _____ ___-285-This paper is for Chinese country Standard (CNS) A4 specification (210X297 mm) --------- Approved clothing ------ 1T -----, hl ^., 1 .... (Please read the back Attention V (Please fill in the back page) The Chinese Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs printed No. 83100644 of the Chinese Patent Application Specification Amendment Page (August 1985) A7 B7 V. Description of the invention] 藤 藤 基] -Benzylamine ( (Formula DD-2) is shown in the DD diagram. To 50 mg of the spring 262 title product was added 0.3 ml of DMSO ° mixture was cooled to Ot :, 30 mg of potassium carbonate was added, and the mixture was stirred for 30 minutes. Add 120 microliters of 30% hydrogen peroxide. Warm the mixture to room temperature and stir for 15 minutes at room temperature. Add 5 ml of water and wash the resulting aqueous solution M10 ml of ethyl acetate three times. The resulting aqueous solution K 1 N HC 1 was acidified and the resulting acidic: aqueous solution was extracted twice from 15 ml of ethyl acetate. The ethyl acetate solution was dried over sodium-free, filtered, and evaporated to dryness to give the title product * 6. The physical properties are as follows: White amorphous solid. HRMS: 522. 1853 ° MS (EI): 522, 507, 338, 310, 233, 207, 195, 186, 144, 131, 119, 105, 69, 55 ° TLC ( Silicone GF): Rf = 0.3 (50% ethyl acetate / hexane plus 0.5% ethyl acetate). Example 365B 2H-cyclooctyl [b] piperan-2-methyl, 3- [cyclopropyl [3- (2-isothiazolidinyl) phenyl] methyl] -5,6,7,8,9, 10-hexahydro-4-hydroxy-S, S-dioxide (formula EE-2); N- [3- [cyclopropyl (5,6,7,8,9 "0-hexahydro--4 -Hydroxy-2-oxy-2} 1-cyclooctyl [b] piperan-3-yl) methyl &gt; phenyl] -4-morpholine propanesulfonamide (formula EE-3); and Bu [3- [Cyclopropyl (5,6, .7,8,9,10-hexamouse-4-meryl-____- 286 -___ This paper is compliant with China National Standards (CNS) A4 (210X297) & &Gt; binding line 'J. I. ^ (Please read the note on the back first fill in the # page) No. 83100644 Patent Application Chinese Specification Correction Page (August 1985) A7 ~ B7 V. Invention Description Ministry of Economic Affairs Printing of 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-morpholine propanesulfonamide hydrogenated iodine salt (Formula EE) -4) See EE diagram. To 96 mg of the title product of Example 331 was added 2 ml of acetonitrile, 34 mg of sodium iodide and 26 µl of morpholine. The reaction mixture was heated under a loop for 24 hours. The reaction mixture was cooled to room temperature * And evaporated to dryness under vacuum to produce a crude foam. The substance was dissolved in a small amount of dichloromethane and chromatographed on silica gel. K 50% ethyl acetate / hexane was first used. "Following 5% methanol / chloroform can produce three title products. — The physical properties of the first title product are as follows \ White amorphous solid. HRMS: 443.1766 ° MS (EI): 443, 415 233, 220, 207, 184 TLC (silicone * GF): R-The physical properties of the second title product are as follows: white non-crystalline solid. HRMS: 530.2444 ° MS (EI): 530, 513, 499, 487 148, 128, 100, 70, 56, 40 ° TLC (silicone, GF): Rf = 0.3 (15 ^ methanol / chloroform) Physical properties of the third title product The following is a light yellow solid. HRMS: 530.2447 〇402, 379 172, 158 350, 322, 291, 250, 129 〇0.15 (50% ethyl acetate / hexane). 338, 307, 192, 158, this paper Standards are applicable to Chinese national standards (CNS) A4 specifications (2 丨 〇X 297 mm) I—I binding I order—line .... (Please read the notes on the back to complete this page first) Central Standards Bureau, Ministry of Economic Affairs Employee Consumer Cooperative Co., Ltd. Printed the Revised Page of the Chinese Specification for Patent Application No. 83100644 (August 85) V. Description of Invention (&gt; &lt;%) MS (EI ): 530, 499, 487, 338, 192, 100, 70® TLC (silicone GF): Rf = 0.33 (15% methanol / chloroform). Spring Example 366 Thiourea, N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro- 4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -N'-phenyl- (Formula V-2 * where Ri is phenyl) see Figure V. In a flame-dried 10 ml two-necked flask, 'dropwise under nitrogen Add phenyl isothiocyanate (0.039 g) to the title compound of Example 164 (0.1 00 g) in 1 ml of CH3CN, and stir the reaction mixture at a constant temperature for 24 hours. The crude reaction mixture was chromatographed on a 25 g silica column to give 0.118 g of the title compound as a solid. The physical properties are as follows: HP 120-123¾ ° IR (Nujol) 3188, 3074, 3060, 3028, 2994, 2953, 2922, 2855, 1664, 1630, 1599, 1591, 1545, 1498, 1492, 1464, 1446, 1406, 1376 , 1357, 1314, 1295, 1252, 1231, 1201, 1172, 1126, 695 cm-1. HS (FAB) m / z 949, 551, 497, 475, 382, 340, 338, 281, 247, 94 〇 High resolution measured value: 475.2064. Example 367 Sulfur gland, N- [3- [cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy-2-2--cyclooctane [b] piperan-3 -Methyl) methyl] phenyl] -ΙΓ-ethyl- (Formula V-2, of which is ethyl) see V chart ____________ — 2 8 8 ~ This paper size is applicable to China National Standard (CNS) M specifications ( 210X297 mm〉 ------------- 丨 Installation ------ Order -------- ^ 丨 line ,,, ...; (Please read the note on the back first ^^^ Fill in this page) The Chinese Consumers 'Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs printed No. 83100644 of the Chinese Specification for the Patent Application (August '85) A7' B7 V. Description of the invention (prepared according to the above example 366). 0.200 g of the title compound was isolated as a solid. The physical properties are as follows:: MP 105-107 T: 13C HMR (DMS0) δ 180.0, 165.1, 163.9, 161.7, 144.0, 136, 2, 130.0, 126.4, 124.4, 122.7, 110.3, 105.7, 44.4, 40.3, 30.8, 29.1, 28.8, 26.1, 25.7, 22.2, 14.1, 12.8, 5.6, 4.1 ppm .0 IR (N uj ο 1) 3217, 3074, 3063, 2995, 2954, 2923, 2868 , 1664, 1665, 1631, 1606/1 588, 1542, 1487, 1461, 1453, 1405, 1376, 1336, 1 309, 1279, 1248, 1226, 1202, 1 17 2, 1 1 2 6 cm-1. MS (ΕΙ) π / ζ 426, 381, 353, 352, 340, 233, 220, 207. Example 368 Phenylthiolamine, hydrazone- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzene Base]-(Formula W-2) See Figure W. In a flame-dried flask, add 1.9 ml of toluene under nitrogen to Example 2 07. The title compound (0.200 g) and Lawson's reagent (0.177 g>) The reaction mixture was refluxed for 1.5 hours, cooled in an ice bath to induce precipitation. The solid was collected from the filter and dried under vacuum at 60 to give 0.111 g of the title compound. MP 163t: 13C NMR (DMS0) δ 201.3, 165.6, 164.3, 161.3, _'___- -__ This paper size applies to China National Standard (CNS) A4 (210X297 mm) (Please read the precautionary order on the back before filling #page). Installation · -e Printed Chinese Manual of Patent Application No. 83100644 by the Consumer Standards of the Central Standards Bureau of the Ministry of Online Economics Amendment Sheet (August 1985) A7 ~ B7 V. Description of Invention 141.9, 138.8, 13 4 .. 8, 129.5, 129.3, 129.3, 128.0, 126.5, 123.3, 122.0, 110.8, 105. 7, 54.8, 43.7, 30.7, 29.1, 28.8, 26.1, 25.8, 22.1, 13.0, 4.9, 3.8 ppm 0 IR (Hujol) 3304, 2953, 2925, 2870, 2854, 1660, 1646, 1593, 1559, 1552, 1533 , 1482, 1466, 1456, 1437, 1393, 1381, 1237, 1199, 1123, 737, 700 cm_1. MS (ED m / z 473, 440, 281, 280, 227, 226, 134, 1 28,91, 55 ° Preparation 59 Phenyl-1-butanase (Formula U-2, where 1U is propyl) See Figure li. Following the general method for the preparation of 54 without significant changes, but the replacement of isopropylphenyl hydrazone with Kpropylphenyl ketone gave 1.52 g of the title compound as a colorless oil. Physical properties are as follows: XH NMR ( CDC13) 5 7.30, 4.68, 1.81-1.62, 1.45- 1.23, 0.93 ppm ° Examples 369 5, 6,7, 8,9,10-Hexa-4-hydroxy-3- 3-U-phenylbutyl) -2H -Cyclooctyl [b] piperan-2-one (formula ϋ-3 * where propyl is propyl)-see U figure. Following the procedure of Example 107 without significant weight change, but replacing the cyclopropylphenyl group with the title product of K Preparation 59, 698 g of the title compound were obtained as a white solid. _____ = ~ 2-9-0 ~ — This paper size applies to China National Standard (CNS) A4 (210X297 mm)

丨 .-------- Binding ^ (Please read the note on the back 背面 and then fill in this page) I The printed page of the Chinese manual for the patent application No. 83100644 printed by the Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs ( August 1985) A7 _ B7 V. Description of the invention (&gt; 0) Physical properties are as follows: HP 173-175¾ 〇IR (Hujol) 3158, 2954, 2924, 2855, 1663, 1638, 1563, 1463, 1408, 1376, 1189 , 1175, 1110, 699 cm_1. Preparation of 60 amino formic acid, [3-U-hydroxy-2-methylpropyl) phenyl] -phenylmethyl ester (Formula X-2) See X diagram. Following the method of preparing 49-52 without significant changes, but K isopropyl benzophenone replaced cyclopropylphenyl, and 698 g of the title compound was obtained as a white solid. ^ Physical properties are as follows: MP 99-1 02¾ 〇ΧΗ HMR (CDC13) 6 7.42-7.24, 7.02, 6.68, 5.20, 4. 3 5, 1. 9 4, 1. 7 5, 0.9 7, 0 · 8 0 ppm . 13C HMR (CDC13) 5 153.2, 144.8, 137.6, 135.9, 128.8, 128.5, 128.3, 128.2, 121.6, 117.6, 116.7, 79.6, 66.9, 35.1, 18.9, 17.9 ppm 〇IR (Hujol) 3432, 3277, 2963, 2954 , 2924, 2866, 2856, 1700, 1602, 1561, 1467, 1447, 1284, 1256, 1240, 1068, 1028, 798, 739, 697 cm-1. Elemental analysis found: C, 71.89; -H, 7.20; N, 4.83. MS (El) m / z 299, 256, 212 ^ 91 °. Measured value at high resolution: 299. 1524. Example 370 [3- [Bu (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-291- This paper size applies to Chinese National Standard (CNS) A4 specification (210 × 297)厘) Binding. ~ Thread (please read the notes on the back ν.ίφ to complete this page) Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 8310064 No. 4 Patent Application for Chinese Manual Revised Page (August 85) A7 ~ B7 V. Description of the invention (-2H-cyclooctyl [b] piperan-3-yl) -2-methylpropyl] phenyl] -aminocarboxylic acid, stupid methyl ester (formula X-3) see Figure X. Following the method of Example 107 without significant changes, but preparing 60 title compound instead of oc-cyclopropylbenzyl alcohol, 0.196 g of the title compound was obtained as a white solid. The physical properties are as follows: MP 96-lOlt: ° XH NHR (CDCl3) 5 7.44-7.IS, -6.70, 6.10, 5.19, 3.87, 2.82, 2.57, 2.43, 1.71, 1.61- 1.36, 0.95 ppm 13C HMR (CDCU) 5 165.0, 163.4, 161.2 , 153.2, 143.4, 138.2, 135.9, 129.5, 128.5, 128.2, 128.1, 123.3, 118. 2, 117. 0, 109.8, 106.0, 66.9, .48.5, 30.7, 29.0, 28.8, 28.1, 26.1, 25.6, 22.1, 21.9, 29.9 ppm 0 IR (Hu jo 1 ) 3300, 2955, 2923, 2866, 2854, 1735, 1698, 1665, 1632, 1609, 1596, 1549, 1494, 1465, 1455, 1446, 1427, 1405, 1383, 1377, 1368, 1335, 1320, 1315, 1219 , 1174, 1086, 1067, 740, 732, 696 cm-1 〇Measured value of elemental analysis: C, 73. 30; -H, 6.87; H, 2.78 ° MS (El) m / z 475, 432, 414 ^ 388, 384, 324, 281, 195, 194, 193, 91 ° Example 371 3- [l- (3-Aminophenyl) -2-methylpropyl] -5,6,7,8, ____ = _〇92 This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) ---------- ^ ------ 1T ----- (Please read the Notes: 1) The printed page of the Chinese specification for the patent application No. 83100644 printed by the Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (δ 1985) = Β7 V. Description of the invention Kf) 9,10-hexahydro-4 · • Jingji-2H-cycloxin [b] Nilan-2-feed (formula X-4) see X diagram. Following the general method of Example 164 without significant changes, but replacing the title product of Example 119 with the title product of Example 370, 1.07 g of the title compound was obtained as a gray solid. The physical properties are as follows: MP 10 5-1101: (decomposed). Example 372 4-cyano-N- [3- [BU (5,2 6,7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctane-3 -Methyl) -2-methylpropyl] phenylsulfenylsulfonamide (X-5 * where the aryl group is 4-cyanobenzene) see X diagram. Following the method of Example 221 without significant changes, but the title product of Example 371 replaced the title product of Example 164, and 4-cyanobenzenesulfonyl chloride replaced 4-chlorosulfonylsulfonium chloride. 0.152 g of the title compound was obtained in white solid. The physical properties are as follows: MP 158-163 C. IR (H uj ο 1) 3127, 3088, 3074, 2956, 2924, 2866, 2 8 5 7, 1 7 0 3, 1673, 1633, 1550, 1466, 1454, 1422, 1402, 1378, 1348, 1284, 1241 , 1221, 1 199, 1185, 1168, 1157, 1091, 734,644 634, 624 cm-1 〇 Example 373 4-Chloro-N-[3-[1-(5,6, -7,8,9 , 10-hexahydro-4-hydroxy2-oxy-2H-cyclooctyl [b] piperan-3-yl) -2-methylpropyl] cyl] benzidine (Formula X-5, where The aryl group is 4-chlorobenzene y See X. _-2-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) --------- installation ------ Order ----- line (please read the notes on the back if you want to fill in this page) A7 B7 Revised Chinese Manual of Patent Application No. 83100644 (August 85) V. Follow Example 221-General method, Without significant changes, but instead of the title compound of Example 164, the title product of Example 371 was replaced with Example 150 to obtain 150 g of the title compound as a white solid. Physical properties such as t: MP 92-95t: (decomposition) IR (Hujol) 3374, 3132, 3096, 2991, 2955, 2923, 2867, 1703, 1695, 1670, 1634, 1605, 1591, 1553, 1378, 1355, 1196, 1172, 989, 829, 1474, 1468, 14 57, 1450, 1409, 1398 1340, 1322, 1298, 1266, 1229, 1214 1164, 1 121, 1095, 1083, ϋ, 1015 774, 754, 730, 608 cm-1. Example 374 1 [3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxyl-211-cyclooctyl [1)] piperan, 3-yl) -2-methylpropyl] benzene Group] -1-methyl-1H-oxazole-4-sulfonamide (Formula X-5, in which the aryl group is 1-methyloxazole) is shown in the X diagram. Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs of the National Standards of the People's Republic of China I with a moderate ruler-paper A6 B6 Printed by the Shell Consumers Cooperative of the Central Standards Bureau of the Ministry of Economics 5. Explanation of the Invention (293) Embedded Examples The general method of 2 21 without major changes, but replacing the product of title 164 with the product of example 371, and replacing 4-benzylbenzenesulfonium with methylmethyl-4-sulfonyl chloride, can obtain 0.125 G of the title compound was a white solid. The physical properties are as follows: MP 143-147Ό (decomposed). Preparation 61 (3-Benzaldehyde) _aminocarboxylic acid, phenylmethyl ester (formula 2) see Figure Y. 0 In a flask with a nitrogen inlet, add sodium bicarbonate (1.04 g) in 20 ml of THF and 20 ml of water. Then, add meta-aminobenzaldehyde (1.0 g) and benzyl formate (1.77 ml) in this order. The mixture was stirred at room temperature for 40 minutes. Ether was added, and the organic layer was separated, washed with M saturated HaHC03, dried over Na2S04, filtered, and concentrated to give a brown oil. Upstream column chromatography on 600 g of silica gave 1.61 g of the title compound as a pear-like solid. The sample for analysis was recrystallized from ethyl acetate-hexane. The physical properties are as follows: MP 100-104 = ° IR (Hujol) 3269, 2954, 2925, 2868, 2855, 1729, ·, · '1682, 1597, 1560, 1465, 1455, 1445, 1326, 1294, 1237, 1229 , 1170, 1155, 1048, 695 cm-1 ° MS (El) m / z 255, 21 1, 91 〇 High resolution measured value: 255.Q900. Preparation 62 [3- (1-hydroxybutyl) phenyl] -aminocarboxylic acid, phenylmethyl ester (Formula Y-3, where IU is propyl) See Y diagram. Install ............ Order ............ line {Please read the precautions on the back before filling (This page) -295- This paper uses the Chinese National Standard (CNS) A4 Specification (210X297mm) No. 831 00644 Patent Application Chinese Revision Book (August 85) A7 B7 V. Invention Description (A 50 ml three-necked round bottom flask with a nitrogen inlet, add the title product of Preparation 61 and 15 ml of THF. Add propylmagnesium (2.2 ml &gt;), and search the resulting mixture for 18 at room temperature. Hours. Add saturated NH4C1, and partition the mixture into ether and water. Wash the organic layer K4N Ha 0H. The alkaline wash solution was acidified with M4H HC1 and extracted with ethyl acetate. The ethyl acetate layer was evaporated to give 1.2 g of oil. Gram silica gel column chromatography can produce a pale yellow oil, which is crystallized from ethyl acetate-hexane to produce 0.35 g of the title product as a white crystalline solid. Physical properties are as follows: MP 103-106 ^… IR (Hujol) 3396, 3249, 3208, 3101, 3082, 3068, 29 50, 2927, 2870, 2863, 2857, 1695, 1602, 1568, 1465, 1448, 1306, 1279, 1256, 1244, 1174, 1068, 1037 772, 736, 694 cm. Example 3 7 5 [3- [Bu (5, 6, 7, 8, 9, 10-hexahydro- 4-hydroxy--2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) butyl] phenyl] · -aminocarbamic acid, phenylmethyl ester (Formula Y-5, where h is propyl) See Y Figure 〇 Printed by the Consumer Consumption Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs The general method of Example 107, without significant malting, but the title product of κ system Jun 62 replaced α-cyclopropylbenzyl alcohol to obtain δ13 g of the title compound as a beige solid.-The physical properties are as follows:. MP 64-67 = 0. Example 376 3- [1- (3-Aminophenyl) butyl] -5,6,7,8,9,00-hexahydro_ This paper size applies to Chinese National Standards (CNS) A4 specification (210X297 mm) Revised Chinese Manual of Patent Application No. 83 100644 printed by the Employees' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (August 1985) V. Explanation of the invention 4-Hydroxy-2H-cycloxin [b] Piperan-2-one (Formula Y-6, where iU is propyl) is shown in Figure Y. The general method (M-7) of Example 164 was followed without major changes, but the title product of Example 375 was used instead of the product of Example 119 To get 0.51 grams of title Brown solid. The physical properties are as follows: &quot; H HMR (CDC13) 5 7.17, 6.83666.71, 6.59, 4.37, 3.73, 2.59, 2888, 2.10- 1.98,:-1 + .95-1.84, 1.75, 1.60-1.33, 0.97 ppbi ° Example 377 sulfasalazine, 4-chloro-N- [3 '-[1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [ b] piperan-3-yl) butyl] phenyl; I- (formula Y-7, in which propyl is 4-propyl and aryl is 4-chlorobenzene) See Y diagram. Following the general method of Example 221 without major changes, but replacing the title product of Example 164 with the title product of Example 376, 0.107 g of the title compound was obtained as a white solid. The physical properties are as follows: MP 97-101: (decomposition). Example 378 besylate, 4- »yl-H- [3-U- (5,6,7, δ, 9,10-hexahydro- 4-Ethyl-2_oxy_2H-cyclooctyl [b] n.an-3-yl) butyl] phenyl]-(formula Y-7-, where "is propyl and aryl is cyanobenzene (See Figure Y): Guangyi follows the general method of Spring Example 221 without major changes, but replaces the title product of Example 164 with the product of Example 376 and 4-fluorobenzenesulfonyl chloride ____- 297 -_ paper method Applicable to China National Standard (CNS) A4 specification (210X297 mm)

It nil I nnn, 1T, n I. V / ^ I ..... one by one (please read the notice on the back before filling this page) No. 83100644 Chinese Application for Correction of Patent Application (August 85 5. Description of the invention (Substituting 4-chlorobenzenesulfonyl chloride, 0.101 g of the title compound can be obtained as a white solid. The physical properties are as follows: MP 130-135t ° Example 379 3- (α-cyclopropylthiophene-2-ylmethyl) Group) -4-hydroxy-5,6,7,8,9,10-hexahydro-cyclooctyl [1〇] piran-2-_ (formula 卩 卩 -3) see FF diagram 0 for formula FF-2 A solution of 2H-cyclooctyl [b] piperan-2-one (1.94 g) and α-cyclopropylthiophen-2-ylmethanol (1.54 g) in methane. Add 5 drops of trifluoroacetic acid at room temperature. (TFA). Re-stirring for J | _15 hours. Add HgStU and over-react and evaporate K to form a yellow oil. This is dissolved in 25% EtOAc / hexane * and placed in the refrigerator to generate 2.5 g of impure after mashing. Title product. Chromatography on silica gel (2% methanol / dichloromethane) yielded 830 mg of the pure title product. The physical properties are as follows: IR (mull) 2953, 2923, 1657, 1631, 1552, 1531, 1464, 1223, U 98, 11 87 cm-1; Mass spectrum: m / z (relative intensity) 330 (99), 313 (1 3), 302 (13), 301 (15), 207 (27), 204 (15), 137 (25), 97 (18); (Please read the notes on the back first and fill in this page). 11 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy H-NMR (CDC 13) 7 .3 (d, 1H), 7 .2 (m, 1H), 7.0 (m, 1H),, 4.1 (d , 1H), 2.6 (π, 2H), 2.4 (m, 2Η), 1.7 (m, 1H), 1.5 (m, 4H), 0.7 (B, 1H), 0.6 (m, 2Η) t 0.4 (m, 1H). W ~ Preparation of 63 ethylthiophene-2-ylmethanol (formula GG-2) see GG diagram. 1.0 M solution of ethylmagnesium bromide in THF (100 ml) &lt; 丨 cooling To -78 -298-This paper size is applicable to the Chinese National Standard (CMS) A4 (210X297 mm) Printed on the Chinese Manual for Patent Application No. 83100644 by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) ) A7 _ B7 5. Description of the invention t, and add 2-thiophene carboxaldehyde (9.35 ml). Allow the reaction to warm to 23t! For 1 hour, then cool to -78 spoons, and stop by adding ammonium chloride. After warming to 23¾, the reaction was extracted with ether (800 mL), and the ether layer was washed with water (2 × 150 mL) and brine. The organic layer was dried over MgS04, dried and vacuum concentrated. Product K silica gel Purified by column chromatography (2 kg), K 30% ether / pentane was dissolved, and 13.4 g of the title product was obtained in the form of a colorless hydration. The physical properties are as follows: HHR, 300 HHz (CDC13) 5: ^ -7.24 (m, 1 Η), 6.96 (nt, 1 Η), 4.84 (nt, 1 Η), 3.37 (m, 2 Η), 2.21 (d, J = 3.6 Hz, 1 Η), 1.83 (br sVl Η), 0.96 (t , J = 7.5 Hz, 3 H) ° Example 3δ0 3-U -Ethylthiophen-2-ylmethyl) -4-hydroxy-5,6,7, δ, 9,10-hexahydro-cyclooctyl [b ] Piran-2- 嗣 (formula GG-4) see GG diagram 0 2H-cyclooctane [b] piperan-2-one (388 mg) of formula GG-3 was dissolved in dichloromethane (2.0 ml) and Add 23 ethyl ethylthiophene-2-ylmethanol (450 mg) and fluoroacetic acid (5 drops) at 23 = 0. Stir for 4 hours, then chromatograph on silica gel (300 g), dissolve K1: 1 ether: pentane to give the title product (220 mg) as a white solid. The physical properties are as follows: MP = 163-5Ϊ;-IR (mull): 3171, 2954, 292.3, 2869, 2854, 1662, 1638, 1564, 1448, 1461, 1411, 1189, 1171, 1057, 6 9 4.4 cm_ 1; _______-_ ~ 9 Q ^-__- This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) —----- ^ Packing, ordering (please read the first Note: Please fill in this page again) Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs __B6___ V. Description of Invention (298) UV (EtOH) Amax (E): 210 (22,100), 220 sh (15,400). 234 sh (9,700), 296 (9,200); 1 H NMR (CDCU) 300 MHz, δ: 10.6 (br 1 H), 7.23 (d, J = 5.1 Hz, 1 H), 6.88 (m, 2 H), 4.36 ( dd, J = 6.1, 9.3 Hz, 1 H), 3.34 (m. 4 H), 2.21 (m, 1 H), 2.02 (m. 1 H), 1.63 (m, 2H), 1.54 (m, 2 H ), 1.41 (m, 2 H), 1.35 (m, 2 H), 0.80 (t, J = 7.3 Hz, 3 H); MS (El) m / e (relative intensity &gt;: 318 (36). 290 (19), 289 (100). 261 (13), 153 (10), 137 (22), 125 (28), 97 (24), 55 (16). 40 (21); Analytical measured value: C, 67.72, H, 7..03, S, 10.37. Preparation of 64 ethyl (5-methylthien-2-yl) methanol (formula H (H-2) See HH chart. 5-methyl-2-thiophenealdehyde (10.0 g) was dissolved in THF and cooled to -78 scoops. Ethylmagnesium bromide was added dropwise to this solution for several minutes ( 1M / hexane; 80ml). Remove the cooling bath to allow the reaction to equilibrate at room temperature. The reaction is stopped by adding saturated NH4C1 solution M. The reaction M is extracted with ether, dried and evaporated to give the title product as an almost colorless oil. The physical properties are as follows: "&quot; IR (mull) 3374, 2964, 2921, 2875, 1462, 1454, 1408, 798 cm-1; H-HMR (CDCla) 6.73 (d. 1H), 6.59 (m, 1H ), 4.72 (t, 1H), 2.45 (s, 3Η), _2 · 05 (s, 1H), 1.80 U, 2H), 0.94 (t, 3H). Mass spectrum: ions at ra / e (relative intensity) 156 (3), 141 (6), {Please read the notes on the back before filling in this page} •• 300 * This paper size is in accordance with China National Standard (CNS) A4 specification (210X297 mm) Central Ministry of Economic Affairs Revised page of Chinese Specification for Patent Application No. 83100644 printed by Staff Bureau of Standards Bureau (August 85) V. Description of Invention 140 (40), 139 (99), 127 (21), 123 (6), 99 (12 ), 97 (7), 65 (6) 〇 Example 381 3-U -B (5-methylthien-2-ylmethyl) -4-hydroxy-5, δ, 7, δ, 9,10-hexahydrocyclooctyl [b] piperan-2-one (formula HH-4) see HH diagram. 2H-cyclooctan [b] piperan-2-one of formula HH-3 (96 mg) and a solution of 64 ethyl (5-methylthien-2-yl) methanol (156 mg) in dichloromethane Add a few drops of TFA. The reaction process was followed by T-layer chromatography (TLC silica gel; M. 25% EtOAc / hexane). After a few hours, the reaction was evaporated and the product was collected on the membrane with the help of M ethyl acetate and hexane trickle * to give 22 5.5 mg of the title product. The physical properties are as follows: IR (mull) 2950, 2924, 2869, 1660, 1635, 1564, 141 3, 1 19 2,1 170, 1 1 57 cm-1. H-NHR (CDCU) 6.86 (d, 1H), 6.62 (d, 1H), 4.47 it, 1H), 2.62 (m, 2H), 2.44 (m, 5H), 2.14 (m, 1H), 1.98 U, 1H), 75 (m, 1H), 1.45 (m, 4H), 1. 0 4 (t, 3 H) 〇 Mass spectrum: i ο nsat in / e (relative intensity) 3 3 2 (2 7), 3 0 4 (20), 303 (99), 275 (8), 153 (7), 151 (22), 139 (44), 111 (9), 55 (9). -Preparation of 65 cyclopropylbenzo [b] thiophene-2 &gt; ylmethanol (Formula II-2) See diagram II. Benzo [] 3] thiophene (2.68 g) of formula 11-1 was added to 1 卩 卩 (70 罨 L) and cooled to -78Ό. Add n-butyllithium (1M / hexane, 20 mol) and ________-301-This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) —-------- equipment -Order &quot; &quot; line ----- .. ..I +! (Please read the note on the back first? Please fill in this page) The Central Consumers Bureau of the Ministry of Economic Affairs printed the patent application No. 83100644 Revised page of Chinese manual (δ5 years August) A7 B7 V. Invention description Stir the solution for 1.5 hours. Remove the cooling bath for 30 minutes and return to -78¾. In another K part, cyclopropylcarboxaldehyde (14 g) was added, and the reaction was stopped by adding a saturated HiUC1 solution. The reaction was extracted several times with ether, and the solvent was removed under dryness and vacuum. The title product was obtained as a clear oil, which could be cured after standing. The physical properties are as follows: IR (mull) 3296, 3201, 2954, 2925, 2869, 2854, 1459, 1438, 1270, 1258 cm-1 ”-H-KMR (CDCla) 7.79 (m, 1H_), 7.7 0 (m, 1H), 7.30 (m, 3H), 4.26 (d, 1H), 2.39 (s, 1H), 1.35 (m, 1H), 0.65 (in, 1H), 0.55 (m, 1H), 0.49 (m, 1H) «Mass spectrometry: ions at m / e (relative intensity) 204 (75), 176 (63 &gt;, 163 (29), 160 (27), 147 (54), 135 (99). Spring example 382 3- ( α-ethylbenzo [b] thien-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one (formula II -4) See picture II. 2H-cyclooctyl [b] piperan-2-one of formula II-3 (196 mg) and cyclopropylbenzothiophene-2-yl methanol of 65 (204 mg) Add a few drops of TFA to the dichloromethane solution. Stir the reaction at room temperature for 30 minutes. Add a few drops of TFA, react and stir for 30 minutes. The solvent is removed under vacuum, and the resulting solid is dissolved in hot 40% EtOAc / hexane. Medium * juxtaposed refrigerator-overnight. Solids collected on the membrane can produce 257.5 grams of the title product. ^ Physical properties are as follows: IR (mull) 2952, 2925, 2853, 1670, 1656, 1627, _____ = ~ 3-6-2 ~-This paper size applies to Chinese national standards CNS) A4 specification (210X297 mm) ---------- batch of clothes ----- 1T ----- · ;. 〆 /.! (Please read the precautions on the back first ϊτ 务(Fill in this page) No. 83100 &amp; 44 Patent Application Chinese Specification Revised Page (August 1985) A7 ~ ------ --- B7 V. Description of Invention (丨) Staff Consumption of the Central Government Bureau of the Ministry of Economic Affairs Cooperative production of U50 'U28, 1458, 1436, cm-1. H-NMR (CDCU) 7.74 (π, 2H), 7.33 U, 2H), 6.4 (s, 1H), 4.12 (d, 1H), 2.64 (m, 2H), 2.45 (η, 2H), 1.77 (hi, lH), 1.47 (m, 4H), 0.82 (m, 1H), 0.68 (B, 2H), 0.46 U, 1H). Mass spectrum: i 〇ns at m / e (relative intensity) 380 (99), 254 (45), 233 (36), 228 (53), 220 (75), 207 (98), 187 (63), 172 (37), 160 (75), 55 (36). …. Preparation of 66 cyclopropyl (5-hydroxymethylfuranmethyl-2-yl) methanol (formula JJ-2) See J J diagram. Furan methyl alcohol (7.0 g) of formula JJ-1 was added to THF (100 ml) and cooled to -78 £. N-butyllithium (1.6} 4, 98.6 ml) was added dropwise, and after the addition was complete, the reaction was stirred at -781! For 2 hours. The cooling bath was removed for 30 minutes and cooled again to -781C. Then cyclopropanecarboxaldehyde (5.0 g) was added dropwise. Stirring was continued for 30 minutes, and the reaction was stopped with a saturated NH4C1 solution. It was extracted with K ether, dried and evaporated to give a dark oil. Chromatography of 0.80 g of the crude title product on silica gel yielded 0.64 grams of the title product. The physical properties are as follows: H-NMR (CDCU) 6.21 (η, 2Η), 4.53 (s, 2Η) ·, 3.94 9d, 1H), 3.0 (broad, 2H), 1.75 (m, 1H), 0.50 (m, 4H ) ^-Example 383 3- (α-Cyclopropyl (5-hydroxymethylfuranmethyl-2-yl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] Piran-2-Meng (formula JJ-4) is shown in the figure. ___- 303 -_. This paper size is applicable to the Chinese National Standard (CNS) (2l0x297mm) (please read the note on the back first) (Fill in the history and fill in this page again) • Packing. -Order. -Line_Revision of the Chinese Manual for Patent Application No. 83100644 by the Ministry of Economic Affairs of the Central Bureau of Standards of the People's Republic of China. Description of the Invention (Preparation of cyclopropyl (5-hydroxymethylfuran-2-yl) methanol 66 (336 mg) and 2'-cyclooctyl [b] piperan-2-one of formula JJ-3 (427 mg) Disperse in 23 ml of dichloromethane (25 ml) and add trifluoroacetic acid (4 drops). Stir the reaction for 2.5 hours, pour into EtOAc (400 ml), and wash with water (2 × 50 ml) and brine. Dried on MgS04, yellow and concentrated under vacuum to produce a yellow foam. The product was separated by column chromatography. (150 grams of silicone), K 30% EtOAc / CH2CU dissociates, and can produce the title product (275 mg) as a white foam.... Physical properties are as follows: IR (mu 1 1); 2923, 2952, 2854, 1668, 1665, 1557, 1203, 1463, U56, 1408, 1247, 1237, 1446, 1016, 1636 cm-1; UV (EtOH) λ max (E): 215 (23,900), 234 sh (10.800), 292 (8,560 ); NMR 300 MHz, CDC] 3,5: 7.26 (s, 1 H), 6.36 (d. J = 3.1 Hz, 1 H), 6.26 (d, j = 3.1 Hz, 1 H), 4.57 (s, 2 H), 3.98 (d, J = 8.1 Hz, 1 H), 2.62 (br t, J = 6.1 Hz, 2 H), 2.49 (br t, J = 5.8 Hz, 2 H), 1.75 (la, 3 H), 1.60 (m, 2 H), 1.47 (m, 4 H), 1.26 (i, 1 H), 0.57 (m, 3 H), 0.29 (b, 1 H); MS (El) m / e (Relative strength): 326 (81), 297 (27), 174 (100), 133 (28), 105 (27), 9-1 (37), 79 (29), 55 (51), 42 (28 ), 40 (38); Analytical measured values: C, 70.08, Η, 6.97. ______ ~ 3 0 4 ~ ____ This paper size applies to Chinese National Standard (CNS) Α4 specification (210 × 297 mm) (Please read the notes on the back ^ '' before filling in this page). Install. 1T A6 B6 V. Description of the invention (303) Preparation of 67 cyclopropyl (5-hydroxymethylthiophen-2-yl) formazan (Formula KK-2) See KK diagram. Formula 1 ([(-1-2-thiophene methanol (5.2 ml) at 1 '} ^ (50 ml), cooled to -78t :, and added n-butyl lithium (Aldrich, 1.6 M / hexane, 73.4 ml) And the reaction was warmed to Ot: 15 minutes. The reaction was cooled again to -78 t: and cyclopropanecarboxaldehyde (4.2 ml) was added. The reaction was warmed to Ot: 30 minutes. The reaction was stopped with aerated ammonium (30 Ml), and then extracted with ethyl ether (400 ml), and then washed with water (120 ml) and brine. The organic layer was dried on MgS04, dried and concentrated in vacuo. The residue was subjected to silica gel column chromatography (1 kg). The title product (5.35 g) can be formed by dissolving with 70% ether / alkane (30%), which is a light yellow oil and can be slowly crystallized. The physical properties are as follows: IR (neat film): 3403, 3004, 2873, 1374, 1289 , 1271, 1214, 1160, 1133, 1096, 1026, 965.4, 939.3, I. 919.1, 810.1 cm-1; (Please read the notes on the back before filling this page} Install the order of the Ministry of Economic Affairs Printed UV (EtOH) Xmax (E): 216 sh (2790), 240 (9870); XH NMR 300 MHz, (CDC 1 3) 3: 6.89 (in, 2 Η), 4.81 ( s, 2 Η), 4.20 (d , j = 8.3, 1 H), 2.22 (brs, 1 Η), 1.28 (m, 1 H), 0.64 (m, 2 H), 0.52 (ia, 1 H), 0.40 (m, 1 H) ; MS (El) m / e (relative intensity): 157 (30), 149 (37), 139 (37), 137 (32) 97 (81), 69 (91), 45 (100), 43 (36) ), 41 (5 3); Analytical found values: C, 59.56, hydrazone, 6.63, S, 15.80. Example 38 4 3- (α-cyclopropyl (5-hydroxymethylthien-2-ylmethyl)- -305- This paper adopts Yin National Standard (CNS) Flat 4 Specification (210x297 mm) —- 1-. No. 83100644 Patent Application Chinese Specification Correction Page (August 1985) A7 ~ B7 V. Invention Explanation (yv) 4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one (formula KK-4) see KK diagram. 2Η- (1) Octyl [b] piran-2-hydrazone (200 mg) and cyclopropyl (5-hydroxymethylthiophen-2-yl) methanol (200 mg) prepared in 67, dissolved in dichloromethane (3.0 ml) ). Trifluoroacetic acid was added, and the reaction was stirred at 23 ° C for 90 minutes. The crude reaction mixture was chromatographed on silica gel (150 g) and K EtO Ac was isolated to give the title product (100 mg) as a white foam. The physical properties are as follows::. IR (mull): 2994, 2953, 2923, 2868, 2854, 1664, 1632, 1556, 1463, 1458, 1408, 1377, 1246, 1233, 1202 cm-1; UV (EtOH) λ max (E): 210 (18,600), 219 sh (15,800), 239 (9,330), 294 (7,840); &quot; H NMR (CDCU), 300 MHz, δ: 6.98 (dd, J = 1.4, 3.4 Hz, 1 H), 6.85 (d, J = 3.4 Hz, 1 H), 4.74 (s, 2 H), 3.64 (d, J = 9.2 Hz, 1 H), 2.62 (m, 2 H), 2.48 (a, 2 H), 1.75 (m, 2 H), 1.59 (m, 2 H), 1.46 («, 5 H), 0.73 (m, 1 H), 0.55 (m, 2 H), 0.35 (m, 1 H) ; MS (El) m / e (relative intensity): 342 (100), 247 (50), 207 (66), 190 (57), 167 (41)-, 137 (71), 135 (39), 97 (47), 55 (61), 40 (53); c- Analytical measured values: C, 66.51, H, 7.28. Preparation 68 Cyclopropyl (5- (2-hydroxyethyl) thiophen-2-yl) methanol (formula LL-2) ___________ * 0 fi ~ __ This paper size is applicable to China National Standard (CNS) A4 (210X297) (Central) 1 ^ Binding. (Please read the notes on the back, and then fill in this page) Printed on the Chinese Manual for Patent Application No. 83 100644 by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) A7 ~ B7 _'___ 5. The description of the invention is shown in the LL diagram. 2-Thienylacetic acid (4.51 g) of formula LL-1 was added to THF (75 ml) and cooled to -78t :. Add n-butyllithium (1.6 M, 46.8 ml) dropwise and search for 1 hour after complete addition. The cooling bath was removed for 20 minutes, and the reaction temperature was returned to -78P. Cyclopropylcarboxaldehyde (2.46 g) was then added dropwise and the reaction was warmed to room temperature, and then a saturated solution of HIUC1 was added to stop. The reaction was extracted, dried and the solvent was removed in vacuo to give the title product as a pale yellow oil. The physical properties are as follows: H-HMR (CDCU) 6.85 (d, lH) ;, -6.70 (d, 1H), 4.12 (d, 1H), 3.83 (m, 2H), 3.0-0 (m, 2H), 1.75 (b, 1H), 0.65 (in, 2H), 0.55 (m, 1H), 0.45 (m, 1H). Spring Example 3δ5 3- (α-Cyclopropyl (5- (2-hydroxyethyl) thiophen-2-ylmethyl) -4-Cyclo-5-5,6,7,8,9,10-Hexacyclic Octyl [b] piperan-2_ _ (formula LL-4) is shown in the LL diagram. 2Η-cyclooctan [b] manan-2-one (196 mg) and cyclopropyl (5- (2) -Hydroxyethyl) thiophen-2-yl) methanol (Preparation 68) (198 mg) in dichloromethane, add a few drops of TFA. The reaction was stirred for 1.5 hours, and the solvent was removed under vacuum. The resulting oil was dissolved in 40% EtO Ac / hexane, placed in the refrigerator overnight. The solid was collected on the filter membrane to produce 136.3 mg of the title product. The physical properties are as follows: IR (mull) 2951, 2922, 2868, 2854, 1670, 1637, 1556, 1448, 1273 , 1022 cm-l ·. H-HMR (CDCU) 7.02 (m, 1Η V, 6.76 (d, 1H), .6.43 (s, 1H), 3.97 (d, 1H), 3.85 (t, 2H), 3.03 ---~ This paper is also applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) I- nn I n I Batch Thread, .-i,. ^ (Please read the notes on the back first ^^ Fill in this page) Printed by the Consumers 'Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 8310064 No. 4 Patent Application Revised page of the manual (August 85) A7 B7 V. Description of the invention (t, 2H), 2.61 (π, 2H), 2.46 (m, 2H), 1.76 (m, 2H), 1.46 (m, 4H), 0.75 (m, 1H), 0.6 (m, 2H), 0.45 (b, 1H). Mass spectra: ions at m / e (relative intensity) 374 (71), 344 (43), 329 (40), 315 (13 ), 303 (11), 248 (80), 233 (41), 220 (58), U1 (66), 163. (65). Preparation of 69 methoxymethylfuranmethyl alcohol. Can be used for MM-1 To MM-2. See: Bull. Cliem. Soc. Jpn., 65 (9), 1992, and Zh. Org · Khim · ", -25 (4), 843-6 (Russ), 1989 ° Preparation 70 Cyclopropyl (5-hydroxymethyl (methyl'oxymethyl) furanmethyl-2-yl) methanol (Formula MM-3) See MM chart. Preparation of 69 methoxymethylfuranmethyl alcohol (1.42 G) was dissolved in THF (20 ml) and cooled to -78t; The reaction was degassed in a nitrogen atmosphere and treated with M n-butyllithium (Aid "ich * 1.6 M / hexane, 6.6 ml). The reaction was stirred for 30 minutes. Cyclopropanecarboxaldehyde (0.75 ml) was added and the reaction was warmed to 231 calendars 20 minutes. The reaction was stopped by adding saturated sodium chloride solution (3.0 ml) and stirred for 15 minutes, then extracted with ethyl acetate (400 ml) * and washed with K water (2 × 50 ml) and brine. Organic The layer was dried on MgS04, dried and vacuum condensed. The product was K-passivated with column chromatography (300 g of silica gel), and K 30% ethyl acetate / hexane was dissolved. The title product was obtained as a colorless oil (U0 g). As follows:-IR (Clear film) 3419, 2937, 288l ·, 1212, 1199, 1148, 1100, 1041, 1017, 995.3, 973.1, 946.1, 929.7, -308-This paper size applies to Chinese National Standard (CNS) A4 Specifications (210X297 mm)

I --------- install ------ order ------ line (please read the notice on the back first ^ '-' service needs to be consumed by the staff of the Central Standards Bureau of the Ministry of Economic Affairs of this FC Cooperative printed the revised Chinese manual of the patent application No. 83100644 (August 85) ___ B7 V. Description of the invention ㈠ 919. 1, 799.5 cm -1; UV (EtOH) λ max (E): 223 (11,200); XH NMR (CDCl3) a: 6.29 (d, J = 3.1 Hz, 1 H), 6.26 (d, J = 3.2 Hz, l H), 4.67 (s, 2 H), 4.51 (s, 2 H), 3.39 (s, 3 H), 2.40 (br s, 1 H), 1.33 (m, 1 H), 0.61 (m, 2 H), 0.46 (m, 1 H), 0.36 (m, 1 H); MS ( El) m / e (relative intensity): 109 (17), 105 (19), 85 (100), 82 (17), 81 (45), 79 ^ (-19), 69 (61), 57 (64 ), 55 (21), 53 (18); Anal. Found: C, 61.65, H, 7'71. Example 386 3- (α-Cyclopropyl (5- (2-hydroxymethyl (methoxymethyl) Ether) furanmethyl-2-fluorene) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2-one (formula MM-5) see MM chart. Cyclopropyl (5-hydroxymethyl (methoxymethyl) furanmethyl-2-yl), methanol 70, was dissolved in dichloromethane (15 ml) and 2H-cyclooctyl [ b] piperan-2-one (formula MM-4 Ml. 36 g). Add trifluoroacetic acid (5 drops) to the reaction mixture of 23 t :, react and search overnight. The crude reaction mixture is chromatographed on silica gel (300 g), and M2.5% methanol / Dichloromethane dissolves to produce the title product (1.94 g) as light yellow glass. The physical properties are as follows: IR (thin film): 2927, 2855, 17 2-1, 1696, 1666, 1639, 1563, 1257, 1 203, 1 148, 1 12 &amp;-, 1 102, 1072, 1040, 1 01 9 cm-1. ____- SrOQ— This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X 297 mm) I Seed clothing II Order—line (Please read the note on the back / fill in the nest page again) Printed by the Ministry of Economic Affairs, the Central Bureau of Standards, Λ Η Consumption and Printing Co., Ltd. A6 _______B6 __ 5. Description of the invention (308) UV (EtOH) Ainax (E): 213 (24100), 234 sh (10,600), 292 (8,110); XH HMR (CDC13), δ: 7.37 (s, 1 H), 6.35 (d, J = 3.3 Hz, 1 H), 6.31 (d, J = 3.2 Hz, 1 H), 4.63 (s, 2 H), 4.49 (s, 2 H), 3.97 (d, J = 8.7 Hz, 1 H), 3.37 (s, 3 H), 2.62 (m, 2 H), 2.49 (m, 2 H), 1.74 (m, 2 H), 1.60 (m, 2 H), 1.37 (m, 4 H), 1.26 (m, 1 H), 0.58 (m, 3 H), 0.26 (m, 1 H); MS (El) m / e (relative intensity): 327 (28 &gt;, 326 (69), 298 (12), 175 915), 174 (100), 149 (41 ), 57 (12), 55 (15), 45 (12), 43 (14); Analytical measurements: C, 68.20, H, 7.43. Preparation 71 Methoxymethyl thienyl-2-enzyme (Formula NN-2) See NN diagram. 2-Thienylformase (50 g) of formula NN-1 was dissolved in dichloromethane (400 ml) and added with Hunig's base (84 ml). The reaction was cooled to Ot: and chloromethyl methyl ether (36.6 ml) was added dropwise. The reaction was warmed to 23t: and stirred for 2 hours. No reaction was observed. The reaction mixture was refluxed for more than 2 hours, and almost no reaction was observed with M TLC. A second portion of chloromethyl methyl ether (37 ml) was added and the starting alcohol quickly converted to the desired ether. The reaction M was washed with water (2 X 500 ml), then dried on MgSO4, filtered and concentrated in vacuo to produce a colorless oil. M silica gel (2 kg) was subjected to column chromatography. M 30% ether / pentane was dissolved to produce The title product was colorless (51.78 g). The physical properties are as follows: XH HHR 300 NHz, CDCla δ: 7.30 (m, 1 Η), 7.02 -3X0- In this long-term system, the standard Η® House Standard Rate (CNS) A4 specification (210X297 mm) ... ........................................ ... K ........: Installation ............ Order .........: Line {Please read "Precautions on the reverse side and write this page first") Printed by A6, Shellfish Consumer Cooperative, Central Procurement Bureau, Ministry of Economic Affairs B6___ V. Description of the invention (3〇9) (in, 1 Η), 6.97 (π, 1 Η), 4.72 (s, 2 Η), 4.69 (s, 2 fO, 3. 4 1 (s, 3 Η) . Preparation of 72 cyclopropyl (5-hydroxymethyl (methoxymethyl &gt; thien-2-yl) methanol (formula NN-3) see NH chart. Preparation of 71 methoxymethyl thienyl-2- The yeast (31.5 g) was dissolved in THF (50 ml) and cooled to -78 T: The solution was degassed under nitrogen and n-butyllithium (Aldrich, 1.6 M / hexane, 133 ml) was added. The reaction was at -78. Add cymbals for 1 hour, add cyclopropanecarboxaldehyde (20.9ml), the color changes from extremely dark to pale yellow, and the reaction is warmed to 0C. The reaction is stopped by saturated saturated forceps solution (40ml). Extract with ether (1.5 liters). The ether extract M water (2 X 400 ml) and wash water. The ether solution was dried on MsSiU, filtered and concentrated in vacuo. The product was purified by column chromatography (2 kg of silica gel), K 1: 1 diethyl ether: pentane dissolves to produce 42.4 g of the standard product as a colorless oil. The physical properties are as follows: IR (thin film): 3422, 3004, 2944, 2δ85, 1375, 1212, 1147, 1099, 1042, 1031, 970.2, 939.3, 920.0, 826. 5, 81 0.1. 1 cm-1; 'OV (EtOH) λ max (E): 216 sh (2940), 240 (10,300); 4 NMR 300 MHz, (CDC13) , 5: 6.89 (m, 2 H), 4.70 (s, 2 H), 4.69 (sz 2 H), 4.19 (d, J = 8.2 Hz, 1 H), 3.41 (s, 3 H), 2.20 (br s, 1 H), 1.26 (m, 1 H), 0.64 (m, 2 H), 0.49 (m, 1 H), 0.43 (ra, -311- this paper »scales, using country t national standards (CNS) Y4 specifications (210X297) "(Please read the precautions on the back before writing this trade). Binding. Order 5. Printed Chinese Manual of Patent Application No. 83100644 by the Central Standards Bureau of the Ministry of Economic Affairs (Chinese version) Month) A7 — B7 Invention Description 1 Η); MS (El) m / e (relative intensity): 228 (33), 167 (32), 139 (63), 138 (51), 125 (26), 111 (30), 91 (23), 69 (100), 53 (.23); Analyze measured values: C, 57. 54, Η, 7. 13. Spring Example 38 7 3 -U-Cyclopropyl (5- (2-hydroxymethyl (methoxymethyl ether) thiophen-2-ylmethyl) -4-hydroxy-5,6,7,8,9 , 10-hexahydrocyclooctyl [b] piperan-2-_ (formula 'NN-5) see NN diagram. 2H-cyclooctyl [b] piperan-2-one (3.0 g "and cyclopropyl (5 -Hydroxymethyl (methoxymethyl) thiophen-2-yl) methanol (3.65 g) was dissolved in dichloromethane (5.0 ml), and trifluoroacetate g U3 drops were added.) The reaction was stirred at 23D for 2 hours All the materials ran into the solution and the reaction mixture was pale yellow. The crude reaction was added to a silica gel (400 g) column * and ethyl acetate was dissolved * to give the title product (6.05 g) as a pale yellow foam. The physical properties are as follows IR (Net): 2927, 2855, 1698, 1662, 1632, 1557, 1407, 1247, 1220, 1202, 1171, 1147, Π02, 1071, 1044 cm-1. UV (EtOH) Amax (E): 208 sh (20,700), 209 (20,800), 220 sh (14,600), 241 (10,400), 294 (9,110); XH NMR (CDCU) 300 MHz, 5-: 7.01 (d, J = 4.4 Hz, 1 H), 6.90 (d, J = 3.5 Hz, "4 H), 6.44 (s, 1 H), 4.68 (s, 4H), 3.99 (d, J = 8.7 Hz, 1 H), 3.40 This paper standard applies to Chinese national standards (CNS) A4 specification (210X297 mm) --------- ^ ------ ΐτ ----- ^ — 0 ....... / \; 'I (please first Read the notes on the back ^ '-# · Fill # this page) Printed Patent Application No. 83100644 of the Central Consumers Association of the Ministry of Economic Affairs No. 83100644 Patent Application A7 ~ Chinese Manual Correction Page (August 85) ~ __ ^-5 Description of the invention (Sichuan) (s, 3 Η), 2.63 (ffl, 2 Η), 2.47 (t, J = 6.2 Hz, 2 H), 1.75 (m, 2 H), 1.60-1.36 (m, 7 H ), 0.75 (m, 1 H), 0.59 (in, 2 H), 0.39 (id, 1 H); MS (ΈΙ) m / e (relative intensity): 343 (19), 342 (54), 314 ( 14), 190 (44), 135 (13), 97 (23), 69 (13), 55 (18), 41 (19); Analytical measured values: C, 64.89, Η, 7.01, S, 7.75. Preparation of 73 N-Benzyl ester furan-2-Samine (Formula 00-2) See Figure 00. Furan methylamine (21.97) of formula 00-1 was added to a saturated HaHCO3 solution. Human benzyl ester j (38.5 g) was added portionwise over M5-10. After the addition is complete, the reaction is stirred for 30 minutes, and then diluted with ether. The ether was separated, dried, and the solvent was removed in vacuo. Chromatography of the resulting oil sand gum (dissolved in 25-50% EtOAc / hexanes) yielded 30 g of pure title product * as a colorless oil. An additional 18 g of the title product was isolated as a pale yellow. The physical properties are as follows: IR (mull) 3331, 1706, 1708, 1525, 1455, 1248, 1220, 698 cm-1. H-NMR (CDCls) 7.34 (s, 6H), 6.30 (s, 1H), 6.22 (s, 1H), 5.11 (s, 2H), 4.36 (s, 2H). Mass spectra: ions at m / e (relative Intensity) 231 (0.3), 140 (99), 96 (81), 91 (87), 81 (18), 69 (22), 65 · (17), 53 (12), 41 (12), 3δ- (13). Preparation 74 Cyclopropyl- (5- (N-benzyl ester sulfanmethylamine)) ketone (Formula 00-3) See Figure 00. ____-313 ~ This paper size applies to China National Standard (CNS) Α4 size (210X297 mm) --------- ^ 丨 Installation ------- Order ----- Line: 1〆 .. .I ... (Please read the note on the back ^ Early fill in the poor page). The Central Consumers Bureau of the Ministry of Economic Affairs printed No. 83100644 of the patent application application A 7 ^ Chinese manual amendment page (8 of 1985 (Months) ~ 5. Description of the invention (N-benzyl ester furan-2-ylamine (4.54 g) from P 彳 Preparation 73 and cyclopropane carbonyl chloride (3.05 g) were added to dichloromethane (with stirring). To this mixture was added A1CU (total 5.28 g) (in portions). After the addition was complete, the reaction was stirred for another 30 minutes, and then it was added to ice. The reaction was extracted with dichloromethane and the mixed organic extract K2M HC1 The K dispersion emulsion was washed. The extract was dried and evaporated to form a dark oil. Chromatography on silica gel (K 2 5-50% EtO Ac / hexane) gave 3.2 g of the title product. The physical properties are as follows: TR (mull) 3259 , 2953, 2940, 2925, 1707, 1679, 1655, 1550, 1 524, 1270 cm-1. H-HMR (CDCU) 7.93 (t, 1H, HH), 7.45 (d, 1H), 7.35 (m, 5H ), 6.57 (d, 1H), 5.04 (s , 2H), 4.28 (d, 2H), 2.68 (m, 1H), 0.95 (m, 4H) ° Mass spectrum: ions at m / e (relative intensity) 299 (1), 258 (0.7), 246 (0.2) , 230 (3), 208 (15), 191 (2), 164 (61), 150 (18), 91 (99). Analytical spring measurement: C, 6δ.16; H, 5.70; Η, 4.62. Preparation 75 Cyclopropyl- (5- (N-benzyl ester furanmethylamine)) methanol ethyl ether (Formula 00-4) See figure 00. Preparation 74 Cyclopropyl (5- (H-benzyl ester benzene) Furan methylamine)) ketone (500 mg · g) was added to a 1/1 mixture of THF and ethanol (5 ml). To this solution was added MaBHA (55 mg). The reaction was stirred overnight and then added 1M HC1 Discontinued. The reaction was extracted with K ether, dried and the solvent was removed to produce 500 mg of the title product as a colorless oil. This paper is in accordance with the Chinese National Standard (CNS) A4 specification (210X297 mm) -------- -IMI equipment-(Please read the precautions on the back to fill out this page)

1. 1T Patent Application No. 83100644 printed by the Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs &lt; Chinese Manual Correction Page (August 85) &quot; &quot; (CDC13) 7.3 (b, 5H), 6.18 (m, 2H), 5.10 (s, 2H), 4.32 (d, 2H), 3.56 (d, 1H), 3.45 (q, 2H), 1.25 (n), 1.17 (t, 3H), 0.64 (m, 1H), 0.45 (ih, 2H), 0.23 (m, 1H). Mass spectra: ions at m / e (relative intensity) 329 (0.7), 283 (9), 238 (11), 222 (3), 210 (5), 194 (4), 179 (7), 166 (8) , 148 (45), 132 (21), 107 (45), 91 (99) 02. — Example 388 3- (α-Cyclopropyl (5-(_ N: benzyl ester) limemethyl) furanmethyl -2-.yl) -4-hydroxy-5, Y, 7,8,9,10-hexahydrocyclooctyl [b] piperan-2-hydrazone (formula 00-6) see figure 00. To a mixture of 2H-cyclooctyl [b] piperan-2-copper (196 mg) of formula 00-5 and the title ether (300 mg) in dichloromethane in methylene chloride was added several drops of TFA. The reaction was stirred for 15 minutes. The solvent was removed under vacuum and the resulting oil was separated on silica gel (40% EtAc / hexane) to give 347 mg of the title product. The physical properties are as follows: H-NMR (CDCU) 7.29 (s, 5H), 6.27 (d, 1H), 6.13

Vd, 1H), 5.25 (t, 1H, HH), 5.06 (s, 2H), 4.26 (d, 2H), 3.84 (d, 1H), 2.56 (t, 2H), 2.45 (t, 2H), 1.69 (m, 2H), 1.55 (in, 2H), 1.35 (m, 4H), 0.54 (m, 3H), 0.22 (m, 1H). -Preparation of 76 N-benzyl ester thiophen-2-ylamine 4 formula PP-2) See PP chart. formula? Thiopheneamine (22.6 g) of 卩 -1 was added to the saturated [^ [1 (: 〇3 solution. The paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) -------- ： —Install ------- order ----- line ...... 1 (please read the note on the back to fill in this page) Patent Application No. 83100644, Revised Page of Chinese Specification (August 1985) A7 ~ --___ B7 _ i. Description of Invention (3d Add benzyl ester chloride (34.0 g) in batches within 5-10 minutes. Complete addition After that, the reaction was stirred for 30 minutes, and then diluted with ethyl acetate. The ether was separated, dried, and the solvent was removed under vacuum. The resulting oil was chromatographed on silica gel (dissolved with 1/1 EtO Ac / hexane) to yield 40.2 g of pure The title product is a colorless oil, which will solidify after standing. The physical properties are as follows: IR (mull) 3349, 2927, 2955, 2927, 1684, 1539, 15 2 6, 1456, 1269, 701 cm-1., H -HMR (CDCU) 7.3 (s, 5ΗΚ-7.19 (d, 1H), 6.92 (οι, 2 Η), 5. 1 0 (s, 2 Η), 4.5 $ (d, 2 Η). Mass spectrum: ions at m / e (relative strength) 247 (0.2), 156 (.99), 1 1 2 (22), 108 (1 0), 107 (9), 97 (20), 85 (19), 79 (11), 85 (19), 65 (8), 44 (8). Preparation of 77 cyclopropyl- (5- (N- Benzyl ester thiophene-2-ylamine)) 嗣 (formula PP-3) See PP chart. Preparation of Benzyl ester thiophene-2-ylamine 76 (4.94 g) and cyclopropanecarbonyl chloride (3.12 g) plus Into dichloromethane (with stirring). A1CU (total 3.12 g) was added to this mixture in portions. After the addition was complete, the reaction was stirred for another 30 minutes and poured into ice. Reaction K dichloromethane extraction, And the mixed organic extract M 2N HC1 washes the M dispersion emulsion. The extract is dried and evaporated to form an oil, which will slowly crystallize after standing. Recrystallization from EtOAc / hexane can produce 1.47 g of the title product as a light gray solid. 》 The physical characteristics are as follows: r H-HMR (CDC13) __ ___; _:-= ~~ 34--8 ~~-This paper size is applicable to China National Standard (CNS) A4 specification (2 丨 0 &gt; &lt; 297) ）). Π YI. Thread (please read the precautions on the back before filling in this page) No. 83100644 Patent Application Check A7, Chinese Manual Correction Page (August 1985) 〇 / V. Description of Invention (一 ^ ) Preparation of 78 Cyclopropyl- (5- (fluorene-benzyl ester thiophene- 2-ylamine)) methanol ethyl ether (Formula PP-4) See Pf &gt; diagram. Cyclopropyl_ (5- (fluorenyl-benzylthiophene-2-ylamine)) one (500 mg) from Preparation 77 was added to THF $ ethanol (5 ml) in a 1/1 mixture. To this solution was added NaBfU (51 mg). The reaction was stirred overnight and stopped by adding 1H HC1. The reaction was extracted with ether, dried, and the solvent was removed to give 500 mg of the title product as a colorless oil. The physical properties are as follows: H-NHR (CDCLa) 7.20 (s, 5Η:)-, · 6.66 (s, 2H), 5.40 ft, 1 H), 4.98 (2 H), 4.34 (_d, 2 H), 3.70 ( d, 1 H), —. 3.34 (m, 2H), 1.07 (t, 3H), 0.52 (ra, 1H), 0.8 (m, 2H), 0.16 U, 1H). Example 389 3- (α-Cyclopropyl (5- (N-benzyl ester) aminemethyl) thiophen-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexa Hydrocyclooctyl [b] Neba-2-one (formula pp-6) See PP diagram. Printing of 2H-Cyclo [b] piran-2- 嗣 (150 mg) of PP--5 and Cyclopropyl (5- (H-benzyl ester) for the production of 78 Thiophene-2-ylamine))-methanol ether (500 mg) To a mixture of dichloromethane (5 ml) was added a few drops of TFA. The reaction was stirred for 5 minutes, the solvent was removed under vacuum, and the crude oil was chromatographed on silica gel (40% EtOAc / hexane) to give 163.1 mg of the title product. The physical properties are as follows: H-HMR (CDC) 3): 7.31 (s, ^ H), 6.92 (d, 1H), 6.78 (d, 1H), 5.31 (t, 1H), 5.09r (s, 2H), 4.43 (d, 2H), 3.86 (d, 1H), 2.60 (t, 2H), 2.48 (t, this paper size applies to China National Standard (CNS) A4 size (210XM7 mm)) Cooperative printed the revised Chinese specification of Patent Application No. 83100644 (August 85), ______ V. Description of Invention (/) 2H), 1.74 (®, 2H), 1.3 (m, 6H), 0.70 (m, 1H ), 0.5 3 (in, 2H), 0.3 7 (m, 1H) 〇 Mass spectrum: i ο nsat ra / e (relative intensity) 4 9 3 (5), 4 0 2 (16), 358 (10), 342 (38), 329 (38), 314 (7), 299 (7), 276 (5), 250 (47), 207 (13), 190 (14), 177 (19), 164 (18), 13 5. (13), 91 (99). Preparation 79 5 -U-Cyclopropyl-1-hydroxy) -2-furanmethylamine (Formula QQ-2) See QQ diagram. To a flask containing 5.0 grams of a solution of QQ-1 furfuryl formamidine in 150 ml of THF, slowly add -67.6 ml of 1.6 M n-butyllithium-hexane at -70 t: nitrogen atmosphere. An alkane solution. The dark brown solution was stirred at -78P for 1 hour * and then treated with 4: 2 5 ml of cyclopropanecarboxaldehyde. At 01: continue to stir for 2.5 hours. The reaction mixture was treated with saturated ammonium chloride and the volatiles were removed under reduced pressure. The residue was partitioned between ethyl acetate and water. The organic layer was washed with brine, dried (magnesium sulfate) and concentrated under reduced pressure. The residue was adsorbed on silica gel and subjected to flash chromatography with 20% methanol / dichloromethane to produce 240 mg of the title product as a brown oil. The physical properties are as follows: ^ NMR (CDC1S) 5 6.23 (d, J = 3.1 Hz, 1H), 6.09 (d, J = 3.1Hz, 1.H), 4.01 (d, J = 8.4 Hz, 1H), 3.81 ( s, 2H), 1.82 (br s, 1H), 1.35 (m, 1H), 0.65-0.60 (m, 2H), 0.45 (in,-1H), 0.36 (m, 1H) ° Preparation 80 Ν- (5 -(α-Hydroxycyclopropyl "methyl" -furan-2-ylmethyl) 4-fluorobenzenesulfonamide] (Formula QQ-3) See QQ diagram. _—_-311 This paper is applicable to the standard China National Standard (CNS) A4 specification (210X297 male stupid). Binding line (please read the notes on the back and fill in this page) · :: 'Printed by the Consumers Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs No. 83100644 Patent Application Inspection A7 ~ Chinese manual revision page (August 85) β7 V. Description of the invention (Qiao) For 0.120 g of 5- (bucyclopropane-buhydroxy) _2-furanmethylamine (Preparation 79) in 4 ml of dichloromethane In a flask of the solution, 0.12 ml of triethylamine was added under a nitrogen atmosphere. The solution was stirred for 30 minutes, and then treated with 0.16 g of 4-fluorobenzenesulfonyl chloride (in 1 ml of dichloromethane) and a K syringe. The reaction mixture was placed in a chamber. Wet and stir overnight, and pour 100 ml of ethyl acetate. Organic water It was washed with brine, dried (magnesium sulfate), and concentrated under reduced pressure. The residue was adsorbed to silica gel and subjected to flash chromatography with 5% methanol / dichloromethane to obtain 199 mg of the title compound in the form of a ochre oil. Physics The characteristics are as follows: "-. HMR (CDC13) § 7.80-7._7_5 (hi, 2H), 7.09-7.04 fm, 2H), 6.05-5.89 (m, 2H), 4.10 (d, J = 5.9 Hz, 2H) , 3.79 (d, J = 8.5 Hz, 1H), 2.94 (br s, 1H), 1.20-1.12 (m, 1H), 0.57-0.49 (m, 2H), 0.45-0.34. (M, 1H), 0.22 -0. 18 (m, 1H); EI-MS: 137 (9999), 148 (9839), 95 (7979), 122 (5619), 69 (4939), 96 (4779), 40 (4089), 121 (3829), 136 (3809), 109 (3739) 〇 Example 390 N- [3- [cyclopropyl (5,6,7,8,9,: 10-hexahydro-4-hydroxy-2- 2-oxo -2H-cyclooctyl [b] piperan-3-yl) methyl] furanmethyl-2-ylmethyl] 4-fluorobenzenesulfonamide (formula QQ-G) see QQ diagram. To a stirred solution of 0.197 g of the title methanol of Preparation 82 in 2 ml of dichloromethane, 0.129 g of cyclooctanone piperane of formula QQ-4 was added under nitrogen, followed by 3 drops of trifluoroacetic acid. The resulting yellow suspension was allowed to stir at room temperature for 2 hours. The reaction mixture was poured into ethyl acetate, and washed with K water, brine, and dried (please read the precautions on the back ^ # fill mouth page)-pack · * order 1 line -------- Q-this paper The standard is applicable to the Chinese National Standard (CNS) A4 specification (210X 297 mm). The printed version of the Chinese specification for Patent Application No. 83100644 printed by the Employees' Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (August 85) 5. Description of the invention (&quot; β Dry (magnesium acetate), filter and concentrate under reduced pressure, adsorb the residue to silica gel, and perform flash chromatography with 30% hexane / ethyl acetate to produce 201 mg of the title product as a white foam. The physical properties are as follows: 1R (mull) 2925, 2953, 2855, 1154, 1666, 1166, 1561 cm-1. UV (95% ethanol) 217. 31600, 295. 8390; NMR (CDC13) 5 7.87 (m, 2H), 7.16 (m, 2H), 6.95 (s, 1H), 6.25 (d, J = 3-.3 Hz, 1H), 6.05 (d, J = 3.0 Hz, 1H), 5.01 (t, _J_ = 6.0 Hz, 1H), 4.15 (d, J = 9.9Hz, 2H), 3.85 (d, J = 8.4 Hz, 1H), 2.78-2.43 (m, 4H), 1.75-1.37 (m, 8H), 1.28 (m, 1H), 0.65- 0.44 (m, 3H), 0.23 (m, 1H); EI-MS: 326 (9999), 174 (5999), 95 (2689), 327 (2419), 161 (2299), 55 (2069), 133 (1909), 271 (1829), 298 (1789), 207 (1659); Elemental analysis found: C, 60.92, H, 5.66, N, 2.66, S, 6.28, F, 4.100. Preparation of SI N- (5-U-hydroxycyclopropylmethyl) -furanmethyl-2-ylmethyl) 4-cyanobenzenesulfonamide] (Formula RR-2) See RR chart. To a flask containing 0.120 g of the formula RR-1 5-U-cyclopropane-1-hydroxy) -2-furan methylamine in 4 ml of dichloromethane, 0.1 2 ml of triethylamine was added under nitrogen. The solution was searched and mixed for 20 minutes under "π, and then 0.15 g of 4-cyanobenzenesulfonyl chloride solution (in 1 ml of dichloromethane) was injected for injection-this paper size applies the Chinese National Standard (CNS) A4 specification ( 210X297 mm) 1 _ ^ ------ 1 — ^, ------ 1Τ ----- ^ _. A '\ ... .. (Please read the precautions on the back before filling in (Pages) No. 831 00644 Patent Application Chinese Specification Correction Page (August 85 ___87_; _ V. Inventor treatment. The reaction mixture was stirred overnight at room temperature and poured into 100 ml of ethyl acetate. Organic matter It was washed with K water, brine, dried (magnesium sulfate), and concentrated under reduced pressure. The residue was adsorbed to silica gel and subjected to flash chromatography at 596 methanol / z; methyl chloride to produce 119 mg of the title compound as a brown oil. The physical properties are as follows : ΑΗ NMR (CDC13) 5 7.87 (m, 2H), 7.71 (m, 2H), 6.05 (m, 1H), 5.95 (m, 1H), 4.19-4.15 (m, 2H), 3.78 (d , J = 8.5 Hz, 1H), 2.87 (br s, 1H), 1.22-1-10 (η, 1H), 0.63-0.48 (m, '' 2H), 0.41-0.33 (m, 1H), 0.24-0.17 (m, 1H); —. EI-MS: 137 (9999), 122 (6-039), 148 (4939), 109 (3999), 121 (3959), 40 ( 3619), 69 (3599), 1.02 (3499), 136 (2859), 26 (2459) ° Examples 391 N- [5- [cyclopropyl (5,6,7,8,9,10-hexahydro- 4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] furanmethyl-2-ylmethyl] 4-cyanobenzenesulfonamide (formula RR-4) see RR chart 〇 Consumption cooperation for employees of the Central Bureau of Standards and Commerce of the Ministry of Economic Affairs (please read the precautions on the back, and then fill in the poor page) 0.117 g of a stirred solution of 81 methanol in 2 ml of dichloromethane * under nitrogen 0.075 g of cyclooctanone piperanone of formula RR-3 was added to the atmosphere, followed by 3 drops of trifluoroacetic acid. The resulting yellow suspension was allowed to stand at room temperature for 2 hours. The reaction mixture was poured into ethyl acetate, and K Washed with water, brine, dried (magnesium sulfate) and concentrated under reduced pressure. The residue was adsorbed to silica gel and subjected to flash chromatography with K30% hexane / ethyl acetate to produce 144 mg of the title product as a yellow foam. -—____- 3 21 This paper size is applicable to China National Standard (CNS) A4 specification (210 &gt; &lt; 297 Gongtu) No. 83100644 Patent Application Chinese Specification Correction Page (August 85) 5. Description of the invention "〆" The physical characteristics are as follows: IR (mull) 2953, 2922, 2868, 2854, 1667, 1561, 1162 cm_1. UV (95% ethanol) 220. 30700, (SH) 235. 21500, (SH) f • Si

279. 7840, 286. 8870, (SH) 293. 8310; J HHR (CDC13) 5 7.96 (d, J = 8.5 Hz, 2H), 7.76 | (d, J = 8.5 Hz, 2H), 6.25 (d, J = 3.3 Hz, 1H), 6.07 f fill (d, J = 3.0 Hz, 1H), 5.15 (m, 1H), 4.22 (m, 2H), f 3.85 («1, 1H), 2.65 (η, 2H ) 2,45 (m, 2H), 1.60 (m, 8H), 1.25 (m, 1H), 0.60 (m ,: 3H), 0.20 (IB, 1H); Elemental analysis spring measurement: C, 62 .26 , H, 5.48, hydrazone, 5. 38, S, 6. 08 0 Preparation of 82 cyclopropyl (5-aminomethylthiophen-2-yl: &gt; methanol (formula SS-2) see SS chart. ( Formula TT -1) See TT diagram. Methylphenamine (0.95 ml) of formula SS-1 is dissolved in: THF (under nitrogen atmosphere) and cooled to -78 ¾. Add n-butyl lithium (Aldr ich 5 1.6 M / hexane, 13.4 ml printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs *) and the reaction turned to dark purple. The reaction was warmed to 10 minutes, then cooled to -78 ^ K and aldehyde (0.82 ml) was added. Formation Thick slurry and made stirring difficult. The reaction was warmed to 0 t :, and then quenched with ammonium chloride solution (10 mL). The reaction was extracted with K EtOAc (200 mL), and Washed with water (2X40 mL) and brine. The organic layer was dried over MgSCU, filtered and concentrated in vacuo. Chromatography (30 ^ 0 g) on silica gel and dissolution with 5% MeOH / CHaC U gave the title product (356 mg ) Is a colorless oil. The physical characteristics are as follows: --------This paper size is applicable to China National Standard (CNS) A4 (210X297 mm). Patent application No. 83100644 printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. Revised Chinese Manual (August 85) B7 V. Invention Description () Small aH NMR 300 MHz, CDCls δ: 6.78 (d, J = 3.5 Hz, 1 H), 6.69 (d, J = 3.6 Hz, 1 H), 4.05 (d, J = 8.2 Hz, 1 H), 3.87 (s, 2 H), 1.18 (m, 1 H), 0.55 (m, 2 H), 0.43 (m, 1 H), 0.28 U , 1 H). Preparation of 83 H- (5- (U-hydroxy) cyclopropylmethyl) thiophen-2-ylmethyl) 4-cyanobenzenesulfonamide (formula TT-2) is shown in the TT chart. Preparation 82 of cyclopropyl (5-aminomethylthien-2-yl) methanol (183 mg) in dichloromethane (5.0 ml) was cooled to 10 t :, and triethylamine (170 µl) was added. Cyanobenzylsulfonium chloride (200 mg) was dissolved in methylene chloride (3.5 ml), and this solution was slowly added to the amine solution. It was stirred at room temperature for 20 minutes, then poured into EtOAc (200 ml), and washed with water (2 x 40 ml) and brine. The organic phase was dried over MsS (U, filtered and concentrated in vacuo to give a yellow oil. * Its M silica gel chromatography (300 g), W5% Me0H / CH2CU dissociation yielded the title product as a colorless oil (284 mg, 82%). ), Which is crystallized from EtAc / hexane as a white powder. The physical properties are as follows: IR (mull): 2924, 1162, 2953, 1334, 2854, 1329, 3260, 3308, 2869, 1456, 1435, 1090, 1442, 1069 cm_1; UV (EtOH) λ max (E): 239 (23,100), 276 (2080), 285 (1620); NMR 300 MHz, CDCls δ:-7.92 (d, J = 6.7 Hz, 2 H) , 7.64 (d, J = 6.6 Hz, 2rH), 6.77 (dd, J = 0.7, 3.5 Hz, 1 H), 6.70 (d, J = 3.6 Hz, 1 H), (Please read the notes on the back first ¾ (Fill in this page again.). Binding. __ 323 — This paper size applies Chinese National Standard (CNS) A4 (210X29 * 7 mm) No. 83100644 Patent Application Chinese Specification Correction Page (August 85) A7 ~ _________B7 __ V. Description of the invention. 5.20 (br », ι H), 4.37 (d, J = 5.6 Hz, 2 H), 2.21 (br 1 H), 1.72 (m, i H), 0.66 (m , 2 H), 0.48 (in, 1 H), 0.37 (m, 1 H); MS (El) m / e (relative intensity): 320 (30), 153 (100), 152 (31), 140 (26), 138 (33), 137 (52), 125 (24), 112 (46), 97 (25), 69 (65); Analytical measured value: C , 54.86, hydrazone, 4.62, N, 7.90, S, 18.20 ° Example 392 H- [5- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4-hydroxy_2-oxyl -2H-cyclooctyl [b] = piperazin-3-yl) methyl] thiophene-2-ylmethyl] 4-cyanobenzene ^ amine (formula TT-4) See TT chart. Preparation of 83-N- (5-((α-hydroxy) cyclo ^ methyl) thien-2-ylmethyl) 4-cyanobenzenesulfonamide (100 mg) and 2H-cyclooctyl of formula ττ-3 [b] Piperan-2-hydrazone (72 mg) was dissolved in dichloromethane (25 g) and trifluoroacetic acid (22 gauge needle, 3 drops) was added. Most of the substance immediately entered the solution, and the reaction became completely homogenized with the addition of 2 drops of trifluoroacetic acid. The reaction was stirred for 10 minutes and then poured into EtO Ac (200 mL) and washed with water (2 × 40 mL) and brine. The organic layer was dried over MgS0 4, filtered, and concentrated in vacuo. The residue was separated on silica gel (100 g) and K 30% hexane / ethyl acetate was used to separate the title product (148 mg) as a white foam. Printed by the staff of the Central Bureau of Standards, Ministry of Economic Affairs, for consumer cooperation (please read the notes on the back, and then fill out this page) The physical characteristics are as follows: IR (mu 1 1): 2923, 2952, 2855, 1 162, 2868, 1667, 1 560, 1338, 1461, 1456, 1 18-3, 1 407, 1447, 1201, 1091, 634.6, 836.1, 1377 cm-1. UV (EtOH) λ max (E): 220 (29,300), 239 (23,800), this paper size applies Chinese National Standard (CNS) A4 specification (21〇 &gt; &lt; 297mm) Ministry of Economic Affairs. Central Bureau of Standards Printed by Employee Consumer Cooperative. Patent Application No. 83100644 A7 ~ Chinese Manual Revised Page (August 85) β7 --------------- V. Description of Invention (3 ^ 279 sh ( 7,790), 287 (8,910), 293 sh (8.590); αΗ HMR 300 HHz, CDCla δ: 7.94 (dd, J = 1.8, 6.7 Hz, 2 H), 7.78 (dd, J = 1.9, 6.7 Hz, 2 H ), 6.85 (dd, J = 1.4, 3.5 Hz, 1 H), 6.71 (d, J = 3.6 Hz, 1 H), 6.43 (br s, 1 H), 5.42 (t, J = 6.1 Hz, 1 H ), 4.34 (d, J = 6.0 Hz, 2 H), 3.84 (d, J = 8.4

Hz, 1 H), 2.63 (m, 2 H), 2.50 (m, 2, H), 1.76 (nt, 2 H), 1.61 (nt, 2 H), 1.47-1.23 (m, 5 H), 0.70 (m, 1 H), 0.54 (m, 2 H), 0.32 (jn-,-1 H); MS (El) m / e (relative intensity) 3_4_3 (27), 342 (100), 330 (26) , 329 (28), 207 (79), 190 (25), 137 (28), 135 (24), 102 (23), 55 (20); Analytical measured values: C, 61.17, H, 5.82, N, 5.23, S, 11.57. Preparation of 84 H- (5-((a-hydroxy) cyclopropylmethyl) thiophen-2-ylmethyl) -4-fluorobenzylsulfonamide (formula SS-3) See SS chart. Cyclopropyl (5-aminomethylthiophene-7-yl) methanol of the formula SS-2 (183 mg) was dissolved in dichloromethane (25 ml) * and triethylamine (170 µl) was added. The reaction was cooled to Ot :, and a solution of sulfamate (194 mg) in dichloromethane (2.0 ml) was slowly added. The reaction was stirred at Ot: for 1 hour and then at 23t: for 1.5 hours. The reaction was poured into EtO Ac (200 mL) and washed with M water (2 × 40 mL) and brine. The organic layer was dried over MgSCU, filtered and concentrated in vacuo to give a yellow oil. The product was chromatographed on silica gel (150 g V, M 5% MeO Η / CH2CU was dissolved. The product was crystallized from EtOAc / hexane to produce _ __- 325-This paper size applies to China National Standard (CNS) A4 specifications (210X297 Mm) --------- ^-Binding I ^ 7, t ......... i /-'f ... (Please read the notes on the back first and then fill in (This page) Printed on the Chinese Application for Patent Application No. 83100644 by the Consumer Standards Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs, Revised Chinese Manual (δδ, 85) A7 V. Description of the Invention (&gt; w) White crystal (219 mg). : IR (mull): 1165, 2924, 1156, 1330, 3260, 2954, 3310, 2854, 2870, 1596, 1294, 841.0, 1091, 1496, 1433 cm; UV (EtOH) λ max (E): 225 (12,300 ), 236 sh (1 1,300); KMR 300 MHz, CDCU δ · 7.87 (dd, J = 5.0, 8.7 Hz, 2 H), 7.20 (t, J = ^ 8-.6 Hz, 2 H), 6.80 ( d, J = 3.5 Hz, 1 H), 6.72 (d, '' = 3.5 Hz, 1 H), 4.77 (br t, J = 5.5 Hz, 1 H), 4.31 (d, 'J = 5.9 Hz, 2 H ), 4.13 (d, J = 8.5 Hz, 1 H), 2.02 (br s, 1 H), 1.21 (m, 1 H), 0.64 (ra, 2 H), 0.48 (m, 1 H), 0.38 ( m, 1 H); MS (EI) m / e (relative intensity): 1 8 2 (8 2), 1 81 (3 2), 15 3 Π00), 152 (36), 140 (28), 138 (29), 137 (48), 1 12 (70 ), 95 (27), 69 (59); Analytical measured values: C, 52.59, Η, 4.76, Η, 4.03. Example 393 Ν- [5- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] thiophen-2-ylmethyl] 4-fluorobenzenesulfonamide (formula ss-5) is shown in the SS chart. 211-cyclooctyl [13] piperan-2-one (64 mg) of formula 5 $ -4 and hydrazone- (5-((α-hydroxy) cyclopropylmethyl) thien-2-yl of Preparation 84) Methyl) -4-fluorobenzenesulfonamide (100 mg) was dissolved in dichloromethane (25 g), and trifluoroacetic acid-326 was added-This paper size applies to China National Standard (CNS) A4 (210X297 mm) 1 Binding (please read the note on the back first * fill the back page) Printed by A6 __B6__, a shelling consumer cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (325) (3 drops). The reaction was stirred at 23¾ for 45 minutes, poured into EtOAc (200 mL), and washed with water (2X 40 mL) and brine. The organic layer was dried over MgS04, filtered and concentrated in vacuo. The product M was column-chromatographed, separated on silica gel (150 g), and dissolved with 30% EtO Ac / hexane to give the title product (143 mg) as a white foam. The physical properties are as follows: IR (mull): 2924, 2953, 2855, 1154, 1663, 1166, 1559, 1236, 1091, 838.1, 1462, 1456, 1407, 1202, 1494 cm; UV (EtOlOXmax, (relative intensity): 211sh (25,600), 216 (26,800), 242 sh (10,200), 295 (8,950); &quot; H NMR 300 MHz, CDCU δ: 7.87 (in, 2 H), 7.17 (m, 2 H), 6.87 (dd, J = 1.4, 3.6 Hz, 1 H), 6.72 (d, J = 3.6 Hz, 1 H), 5.03 (brt, J = 6.1 Hz, 1 H), 4.29 (d, J = 6.1 Hz, 2 H), 3.87 (d, J = 9.1 Hz, 1 H), 2.63 (m, 2 H), 2.49 (m, 2 H), 1.76 (m, 2 H), 1.65-1.23 (m, 7 H), 0.71 ( m, 1 H), 0.54 (m, 2 H), 0.33 (m, 1, H); ',

I1: I * · MS (El) m / e (relative intensity): 343 (25), 342 (100), 330 (19), 329 (22), 207 (43), 190 (26), 137 (23 ), 136 (17), 95 (23), 55 (21); Analytical measured values: C, 57..37, hydrazone, 5.32, hydrazone, 2.62, S, 11.62 〇 Preparation of 85 cyclopropyl (5-methyl -4-Hydroxymethylthiophen-2-yl) formase (Formula _ Know-This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) (Please read the precautions on the back before filling in the book }-Binding. Binding · Printed in Chinese description of Patent Application No. S3100644 by the Consumers' Cooperatives of the Central Government Bureau of the Ministry of Economic Affairs 箐 Revised Page (August 85) A7 ~ __B7__ V. Description of the Invention Π UI-2) Formula 丨] thiophene-3-methanol (4.56 g) of 1] -1 is added to 1 ′ (100 ml), and cooled to -78 t °, then n-butyl lithium (55 ml) is added and the reaction is at- Search and stir at 781 for 2 hours, then remove the cooling bath for 30 minutes. The reaction temperature is again reduced to -78¾. Then add M-cyclopropylcarboxaldehyde (2.8 g), and continue to search and stir for 30 minutes. Reaction K Saturated NH4C1 was discontinued and extracted with ether. The ether extract was dried * the solvent was evaporated in vacuo to A light brown oil was formed. Silica gel chromatography (400 g of silicone; Kl / 1 EtOAc / hexane) gave 1.21 g of the title product. II. The physical properties are as follows:-H-HMR (CDCU) 6.82 (s, 1H) , 4.43 (s, 2H), 3.99 (d, 1H), 3.34 (broad, OH), 3.03 (broad, OH), 2.36 (s, 3H), 1.24 (m, 1H), 0.49 (m, 2H), 0.34 (m, 1 H), 0.28 U, 1 H). Example 394 3-U-cyclopropyl (5-methyl-4-hydroxymethylthien-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [ b] Piran-2-one (formula UU-4) see I] U diagram. Diol of Preparation 85 (400 mg) and cyclooctyl piperanone of formula UU-3 (450 mg) were dissolved in 23 T of dichloromethane (25 ml). Trifluoroacetic acid (22 gauge needle * 3 drops) was added and the reaction was stirred for 45 minutes. The reaction was poured into EtOAc (400 mL) and washed with water (2 × 50 mL) and brine. The organic layer was dried over MsSO4, evaporated and concentrated in vacuo. The residue was chromatographed on silica gel (300 g). M30% Et0Ac / CH2CU was dissolved in J to yield the title product (309 mg) as a white foam. _____________- 3 2 8-This paper size is applicable to China National Standard (CNS) A4 (210XW7mm) --------- 11¾ .----------- (Please read first Note on the back # Fill in this page) A6 B6 Printed by the Shellfish Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (327) The physical characteristics are as follows: IR (mull): 2926, 2952, 2854, 1667, 2868, 1555 , 1202. 1463, 1456, 1407, 1230, 1633, 1247, 2994, 1377 cm &lt;; XH NMR 300 MHz. CDCU 6: 7.10 (d, J = 1.4 Hz, 1 H), 6.53 (s, 1 H) , 4.55 (s, 2 H), 3.93 (d, J = 9.1 Hz, 1 H), 2.62 (m, 2 H), 2.47 (m, 2 H), 2.40 (s, 3 H), 1.60 (m, 2 H), 1.47-1.28 (m, 8 H), 0.72 (m, 1 H), 0.58 (m, 2 H &gt;, 0.34 (m, 1 H). Preparation of 86 2-carboxycyclooctanone (formula VV- 1) See VV chart. In 2-ethyl acetate cyclooctane (prepared according to Organic Synthesis Vol 47, _p 20) (16.3 g), 0.51 ^ 0 [1 (160 ml) was added at 01 °. At room temperature After stirring for 3 hours, the reaction was warmed to ambient temperature for 15.5 hours. The reaction was washed with diethyl ether (50 ml) and hexane (50 ml), and the aqueous layer M UN HC1 was acidified under Ot: precipitation. Collected (K-vacuum filtration method), and washed with M water (3 × 20 mL) and CCU (2 × 20 mL), and M produced 16.8 g of the pure title product. The physical properties are as follows: '. H-NMR Preparation 87 (Formula VV-2 ) See VV chart. To 2-carboxycyclooctanone (16.8 g) of Preparation 86 was added acetone (15 ml), acetic anhydride (20 ml) and sulfuric acid [0.8 ml, and Mot was added dropwise :). Once sulfuric acid was added, The solid is dissolved and ot: do not continue to mix for 1 hour, and the reaction is placed in the refrigerator (4 ° C) overnight. The reaction is poured into Ν3Η (: 〇3ψ (500 ml) -329- This paper uses the standard of t country Standard (CNS) A4 specifications (210X297 male dragon) {Please read the precautions on the back before filling this page)-Binding. I4 ·.

Kh B7 Patent Application No. 83100644 Revised Chinese Manual (August 1985) V. Description of the invention (v /), which contains water, and then stirred at room temperature for 1 hour. The solid was collected on the membrane. It should be washed with water and air-dried to give 0.50 g of product. Recrystallization from diethyl ether gave 8.9 g of the title product. Physical properties are as follows: MP 73.5-4.5t: Example 39 5 3- («[S] -ethylbenzyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctane [b ] Anan-2-one (formula VV-5) is shown in Figure 0. 3 [R] -Phenylvaleric acid (400¾g) of formula VV-3 was added to dichloromethane (5ml), and then grass-chlorine (0.21ml mixed: the mixture was heated under reflux for 3 hours. Dichloromethane decanted Add 1,3,5-trimethyl hen, (10 ml). The solution of the enzyme-based chlorine is heated to reflux temperature, and the title product 87 [VV-2] (210 mg) and triethylamine are added dropwise. (210 mg) (both in 1.5 ml of 1,3,5-trimethylbenzene). After the addition is complete, the reaction is heated for another 3 hours. The reaction is cooled to room temperature and the solids are removed by filtration. The filtrate is evaporated. The resulting residue was diluted with methanol (35 ml) and 0.5N NaOH (4 ml), and the mixture was searched overnight at room temperature. The methanol was removed and water (35 ml) was added. The aqueous layer was ether / hexane (2X 25 ml) extraction * and the aqueous layer was acidified with 1.6H HC1 to rH 3 at 0 = 0. The aqueous layer was extracted with ethyl acetate, dried and the solvent was removed in vacuo to give 318.5 mg of the title product VV-5. On silicone Historical analysis (EtOAc / dichloromethane 1: 8) yielded 49.2 mg of the title product. Physical properties are as follows: MP 201.0-2.0¾. H-NMR 7.36 (m, 5H), 5.8 (s-, OH), 4.36 (t, 1H), 2.60 (t, 2H), 2.40 (t, 2H), 2.16 (in, 1H), 2.04 330-This paper is again free to use Chinese National Standard (CNS) A4 specifications (210X297 mm) Please Precautions for reading first / Special f Printed Chinese Manual for Patent Application No. 83100644 by the Ministry of Economic Affairs 'Central Consumers' Cooperatives (Chinese version) (August 1985) A7 ~ B7 V. Description of Invention (): Central Standards of the Ministry of Economic Affairs Printed by the Bureau's Consumer Cooperatives U, 1H), 1.62 u, 2H), 1.41 (m, 6H), l.oi (t, 3H) Ο C «] D = -156 ° Preparation 396 3- (a [R] -Ethylbenzyl) -4-hydroxy-5, 6,7,8, 9, 10-hexahydrocyclooctyl [b] piperan-2-one (formula WW-5) is shown in the WW diagram. 3 "[S] phenylvaleric acid (400 mg) of formula" -3 was added to dichloromethane (5 ml), followed by chloramphenicol (0.21 ml). The mixture was heated at reflux for 3 hours. The dichloromethane was removed and Add 1,3,5-trimethylbenzene (10 ml). Heat the solution to reflux temperature and dropwise add WW-2 0 and VV-2 (210 mg) and triethylamine (210 mg) ( (1,3,5,3-trimethylbenzene). After the addition is complete, the reaction is heated for another 7 hours. After cooling to room temperature, the solid is removed by filtration. The filtrate Evaporate, dilute the resulting residue K formic acid (35 ml) and 0.5H KaOH (4 ml) and stir the mixture at room temperature overnight. Remove the methanol and add water (35 ml). Water layer ether / hexane (2x 35 ml) was extracted and the aqueous layer was acidified to pH 3 with K1.6N HC1. The aqueous layer was extracted with ethyl acetate, dried, and the solvent was removed under vacuum to yield 287.0 mg of the title product. Chromatography on silica gel (Et〇Ac / dichloromethane 1: 8) can produce 199.4 mg of the title product WW-5. The physical properties are as follows: HP 200. 5-1. 5Ϊ: H-NHR 7.36 (m, 5H), 5.8 (s, OH), 4. 36 (t, iH) 2.δ〇 (t, 2H), 2.40 (t, 2H), -2.16 (m, 1 «), 2.Ο4 (&gt;», 1H), 1.62 (m, 2H), 1.41r (m, 6H), l.oi (t, 3H)

Wl-This paper size is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) (Please read the cautions on the back before filling this page) No. 83100644 Patent Application No. Chinese Specification Revised Page (August 1985) A7 B7 V. Description of the invention [a JD = + 149 ° Example 397 1 [3- [ , 10-Hexahydro-4-hydroxy-2-hydroxy-2Η-cyclooctyl [b] piperan-3-yl> methyl] phenyl] -N-phenylsulfonamide (Formula DDD-3 * where IU is fluorene and R2 is phenyl) See DDD chart. For 52.2 mg of 3-[(3-aminophenyl) cyclopropylmethyl] -5,6,7,8, 9, 10-hexahydro-4 -Hydroxy-2H-cyclooctyl [b] piperan-2-one in 2.0 ml of pyridine * Added 36.7 mg of N-phenylpyridinylamino chloride (according to JA

Kloek; K. L. Leschinsky, J. jo-rg. Chem. (1976) 41: 4028). The solution was stirred for 4 $ _, and then reduced in vacuo. The residue was dissolved in ethyl acetate and water and washed with two cold 5% aqueous hydrochloric acid solutions. The organic layer was dried over sulfuric acid m (NA2S04) and concentrated to give 125 mg of an orange solid. Chromatography on 9 g of 70-230-pore sieve silica gel (K 5% methanol / dichloromethane dissociation) yielded 55.9 mg of the title. The product was a white solid. The physical properties are as follows: MP 90-951C ° Mass spectrum m / z: 495 (M * + H), 340, 207, 186, 144, 93. High resolution mass spectrum: found (m / z) 495.1951 (M * + l). Example 398 H- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -N, N-dimethylsulfonium (Formula DDD-3, where R1 and R2 are methyl) See DDD diagram. -Following the general method of Example 397 above, but using Η, N -dimethylsulfonamido chloride as the sulfonating agent, the title compound can be prepared. -332-This paper size applies to Chinese National Standard (CNS) Α4 ^ (210X297mm) --------- MI equipment -------- Order ----- line (please read the back first Please note that Heng fill in this page again) Printed by the Consumer Standards of the Central Standards Bureau of the Ministry of Economic Affairs No. 83100644 Patent Application Inspection Chinese Manual Revised Page August August) A7 ~ B7 V. Description of the invention ο &); The physical characteristics are as follows: HP 190- 193¾ 〇 Mass Spectrometry® / z: 446 (M *), 418, 405, 360, 339, 322, 311, 294, 233, 207, 195, 186, 144, 130, 117 ° Analytical found values: C, 61.46; Η , 6.75; H, 6.10. Example 39 9 H- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl &gt; Methyl] phenyl] -4-methyl-: l-hexahydropyridazine (Formula DDD-3, where R 1 and R 2 are mixed to form a 4-methyl "hexahydropyridine ring) See DDD Fu 0 follows the method of Example 397, but uses' 4-methylhexahydropyridinesulfonamide. Chlorine (according to WL Matier, WT Comer; D. Deitchman, J. Med. Chem. (1972) 1 5: It is a sulfonating agent described in 538) and can be used to prepare the title compound. The physical properties are as follows: Mass spectrum m / z: 502 (M ++ 1), 391, 338, 324, 241, 177, 163, 149, 99 , 71, 58. High resolution mass spectrometry: measured value (m / z) 502.2398 (M * + l). Preparation of 88 M-phenyl-3- (cyclopropylhydroxymethyl) -benzenesulfonamide (formula BBB) -3, where aryl is phenyl) See BBB diagram. For 970 mg of N-phenyl-3-bromobenzenesulfonamide (easily prepared from commercial 3-bromo-benzenesulfonium) in 55 ml of anhydrous tetra -Hydrofuran solution, add 1.9 ml of 1.6M n-butyl-r-lithium / hexane solution under -781 nitrogen. Stir the solution for 10 minutes, then add 19 ml of n-butyl lithium (1.6M / hexane). Stir the solution -33 3-The size of this paper is applicable to China National Beech Standard (CNS) A4 (210X297mm) -------- "I Pack-.., V '.; (Please read the notice on the back first Qin (Fill in this page)

, 1T line Ministry of Economic Affairs Central Standards Bureau Consumer Consumption Cooperative Printed No. 83100644 Patent Application Chinese Specification Revised Page (August 1985) A7 ~ B7 V. Description of the invention (0 odds and 10 minutes, plus 0.35 ml of cyclopropanecarboxaldehyde The solution was stirred for 15 hours, and then treated with water and ethyl acetate. Solution M 5% hydrochloric acid and brine Kali. The layers were separated, and the aqueous layer was extracted with two portions of ethyl acetate. The mixed organic extracts were sodium sulfate (Na2SCU) Drying and concentrating to form an oil, and chromatography on silica gel (M 5% methanol / dichloromethane) can produce 517 mg (55%) of the title product as a clear oil. The physical properties are as follows: Mass spectrum m / z : 303 W), 275, 2 9, 9, 233, 211, 193, '183, 168, 147, 128, 119, 1 (^, -93, 77, 65. High resolution mass spectrometry: found (m / z) 30 3.0917 (M +). Example 400 H-Appletyl-3- [cyclopropyl (5-, 6, 7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b ] Piran-3-yl) methyl] -benzenesulfonamide (Formula BBB-5) See BBB diagram. P-437 mg of N-phenyl-3- (cyclopropylhydroxymethyl) benzenesulfonamide (preparation 88) in 100 ml of dichloromethane, in molecular sieve 3A Add 282.5 mg of 4-hydroxy-5, S, 7,8,9,10-hexahydro-cyclooctyl [b] piperan-2-one of formula BBB-4, and add 52.0 mg of para-toluenesulfone Acid-hydrate. The reaction was heated to reflux for 1 hour and 30 minutes * and then concentrated in vacuo. The resulting oil was dissolved in ethyl acetate, treated with water and a 1H aqueous sodium hydroxide solution. The layers were separated. Wash with sodium oxide aqueous solution. The mixed aqueous layer was treated with 5% hydrochloric acid in water, and then extracted with three portions of ethyl acetate. The mixed organic mash was dried (sodium sulfate) (Ha2SCU) and concentrated-Μ produced a yellow oil. Chromatography on 80 g of silica gel (K 15% hexane A ethyl acetate dissociation) can produce 74 mg of the substance. This material is chromatographed as above (M50% hexane / ethyl acetate-334-the silver standard of this paper applies Chinese national standards (CNS) A4 specification (210X297mm) ----- II n I. 1— ^ 111 1 VMM— line, ΛΟ · ^. First (if you read the precautions on the back A.-Fill this page) ί Chinese Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs printed No. 8310064 No. 4 Patent Application Chinese Specification Revised Page (August 1985) A7-B7 V. Invention Description Ester Dissolution) May . To 67.3 mg of the title product as a white solid * Physical characteristics are as follows: MP 200-203¾ Mass spectrum m / z:. 480 (M ++ H), 286, 247, 93. High Resolution Mass Spectra: U / z) 480.1850 (tT + 1). Examples 401-411 By using similar procedures as described above, other compounds of the present invention can be prepared under K. Example 401 N- [3- [cyclopropyl (5,6, 9,10-hexahydro-4-hydroxy-2- 2-oxo -2H-cyclooctyl [b] _piperan-3-yl) methyl] phenyl]-(R) -benzylsulfonamide ^ Example 40 2 4-cyano-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4_hydroxy-2_oxy_2H_cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide Example 403 N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -4-dimethylamino) benzenesulfonamide Example 404 4- (bromomethyl) -N- [3- [cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -benzenesulfonamide Example 405 4-[[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [bl · piperan-3-yl) methyl] phenyl] amino] sulfonyl Fluorenyl] -benzylamidine Example 406 N- [3- [Cyclopropyl (5,6,7,8,9,10-Hexahydro-4-hydroxy- (Fill this page)-loaded.

、 5T '^ 线 -335-This paper size is applicable to Chinese National Standard (CNS) A4 specification (2IO × 297 mm) No. 83 1 00644 Patent Application Chinese Specification Correction Page (δ_1985) A7 ~ B7 V. Description of invention 2-oxy-2 [1-cyclooctyl [1)] piperan-3-yl) methyl] phenyl] -5-benzenesulfonyl)-, (S) -2-thiophenesulfonamide Examples 407 N -[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Phenyl]-3-hydroxy-benzenesulfonamide Examples 408 4-butoxy-N- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4 -hydroxy-2 -Oxy- 2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide Example 409 5-chloro-H- [3- [cyclopropyl (: 5-, 6,7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1,3-dimethyl -lH-ώazole-4-lutamine Example 410 2,4-Dichloro-N- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro-4-hydroxy-2 -Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] benzenesulfonamide Examples 411 M- [3- [cyclopropyl (5, S, 7, δ, 9, 10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]-4-hydroxy-benzylsulfonamide I- -^ ------ 7, 丨 Installation -------- Order -----, 'vlu line, .. (Please read the precautions on the back before filling this page) Central Bureau of Standards, Ministry of Economic Affairs Printed by Employee Consumption Cooperatives -336-This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) V. Description of Invention (335) Formula A6 B6

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V. Description of the invention (398) Table I Example number of the compound printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, the actual molecular number of the compound 26 439.1538 27 400.1413 28 399.1495 29 442.1633 30 »513J247 31 365.1621 32 436.1634 33 497.1834 34 292.1094 35 278.0949 36 298.0995 37 324.1357 38 322.1196 | 39 280.1085 40 HC1 salt 295.1213 41 φ 42 494J2427 43 452.1946 44 379 ** cxa 45 400.1426 46 TFA salt 353.1499 47 494.2407 48 TFA salt 394.1885 49 4552089 50 Tuna «51 Fortunate 52 TFA salt 425.1692 53 441.1939 54 455.2087 {Please read the precautions on the back before filling in this page} #.-装. 、 ΤΓ. 400- This paper uses the national standard (CNS) A4 specification (210X297 mm) 5. Description of the invention (399) A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs, the number of compound examples, molecular type, and actual value 55 413.1619 56 433.2248 57 457.1901 58 59 4932313 60 4662099 61 TFA salt 366.1566 62 • 443.1737 63 466.1872 64 477.1935 65 516-1180 66 366 78 366. 1377 79 466.1890 80 286.1201 81 338.1523 82 324.1362 83 276.0997 84 294.1267 86 348.0977 87 298.1017 88 310 89 310 90 294.1268 92 314.0703 93 296.1046 95 296.1043 96 296.1285 97 308.1402 98 305.1067 99 330.1249 ......... ............................................ ....... installed .............. available 丨: r .... ........ (Please read the notes on the back before filling out this page) 401- This paper size is applicable to China National Standard (CNS) A4 specifications (210 parent 297 publications) A6 B6 V. Description of the invention (400) Compound Example Suoning Molecular Type Measured Value 100 370.1418 101 291.0908 103 296.1048 104 256.1105 {Please read the precautions on the back before filling this page)

* MS not obtained * «Low resolution only (no R-peak) *** No FA-B printed by Employee Consumer Cooperative of Central Standards Bureau of Ministry of Economics -402- This paper is applicable to country t ^ CNS) 4 Specifications U10X297 mm) A6 B6 V. Description of the invention (401) Table of compounds printed by the Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Case number HIV protease FITC analysis HIV-1 agent S (uM) HIV-1 protein Sea inhibition% lftv-1 protease 1 ^ 50 (UM) 1 10.000 15.3 20.000 51.62 100.000 66.94, 200.000 92.79 iOO.OOO &lt; 10 2 10.000 15.56 20.000 48.12 100.000 63.56 200.000 97.46 3 1.000 &lt; 10 10.000 &lt; 10 100.000 48.8 4 1.000 &lt; 10 10.000 IZ41 100.000 45.31 5 1.000 15.36 10.000 55.37 100.000 95.01 6 10.000 29.25 20.000 65.61 100.000 88.46 200.000 75.21 7 1.000 &lt; 10 10,000 42.48 100.000 96.33 2U900 8 1.000 &lt; 10 10.000 23.72 100.000 93.35 41.7100 3- (Please read first Note on the back, please fill in this page again.) The size of this paper is applicable to the national standard (CNS) A4 specification (210x297 mm) A6 B6 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (402) Compound S Case No. HIV protein Sea FITC analysis HIV-1 agent M (uM) HIV-1 protease inhibitor% HIV-1 protein plum IC50 (uM) 9 1.000 12.11 10.000 64.99 100.000 98.34 10.5700 10 0.098 &lt; 10 0.196 &lt; 10 0.780 33.22 1.560 53.58 12.500 91.55 25.000 88.03 50.000 101.82 100.000 108.98 1.7100 11 0.098 &lt; 10 0.195 &lt; 10 0.390 19.25 0.780 27.05 1.560 3.130 63.09 6.250 70.36 12.500 82.04 25.000 95 · 77 50.000 90.73 100.000 105.4 1.8900 200.000 107.45 12 0.098 &lt; 10 αι% &lt; 10 0.390 &lt; 10 0.780 13.97 1 ^ 60 17.14 3.130 25.41 .6.250 31.87 {Please read the back first, please note Please fill in this page again for this matter) This paper size is applicable to China National Standard (CNS) A4 specification (210x297 mm) V. Description of invention (40.3) A6 B6 Ministry of Economic Affairs t Central Standards Bureau Employees Consumer Cooperative printed compound instance number ΗΠprotein_FITC analysis of HIV-1 agent (uM) HIV-1 protease inhibitor % HIV-1 protein IC, 0 (uM) 12.500 53.81 25.000 66.55 50.000 74.65 100.000 87.44 12.1000 200.000 87.03! 3 1.000 &lt; 10 10.000 34.68 100.000 74.56 14 1.000 32.21 10.000 64.57 100.000 87.06 15 1.000 43.83 10.000 89.58 1.2500 16 1.000 &lt; 10 10.000 48.32 17! .000 &lt; 10 10.000 27.56 ........... 18 1.000 13.37 _. 10.000 52.54 19 1.000 &lt; 10 10.000 36.79 20 1.000 &lt; 10 10.000 20.33 100.000 79.77 21 1.000 &lt; 10 10.000 12.06 100.000 74.32 74 1.000 &lt; 10 10.000 &lt; 10 100.000 82.28 .............. ......... # .............. t ..... ...........------ 、 may ............ {Please read the notes on the back before filling this page ) I-405- This paper size is applicable to China National Standard (CNS) A4 specification (210x297 mm) V. Description of the invention (40) A6 B6 Compound number printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Example number of HIV protease FITC Analysis of HIV-1 dose (uM)% HIV-1 protease inhibition HIV-1 protease ICjnOiM) 66 1.000 &lt; 10 10.000 &lt; 10 100.000 52.59 67 1.000 &lt; 10 10.000 11.74 100.000 60.91 71 1.000 &lt; 10 10.000 15 100.000 80 68 1.000 &lt; 10 10.000 &lt; 10 100.000 56 36 L000 &lt; 10 10.000 16.89 100.000 81.61 72 1.000 &lt; 10 10.000 18.91 100.000 92.35 37 1.000 &lt; 10 10.000 5955 100.000 102.96 7.0000 38 1.000 18.65 10.000 83.17 100.000 93.37 2.8000 70 1.000 &lt; 10 10.000 10.18 100.000 72.18 73 1.000 &lt; 10 10.000 29.85 100.000 96.66 1 —406— (Please read the notes on the back before writing this page) .β ..........-.............. ^ ....... ..-V. Description of the invention (405) A6 B6 Compound number printed by the Consumers' Cooperative of the China Standards Bureau of the Ministry of Economic Affairs Example number HIV protease FITC analysis HIV- 1 dose of u (uM) HIV-1 protease inhibition% HIV-1 protease (uM) 69 1.000 &lt; 10 10 * 000 20.55 100 * 000 92.22 34 L000 &lt; 10 10.000 50-31 100.000 9U 3.6000 1.000 &lt; 10 16000 10.000 50.31 3.6000 1 00.000 91.1 3.6000 35 1.000 &lt; 10 10.000 19.61 100.000 92.6 6.8000 1,000 &lt; 10 6.8000 10.000 19.61 6.8000 100.000 92.6 6.8000 75 1.000 14.5 10.000 72.66 100.000 96.59 100.000 96.59 2.4000 26 1.000 &lt; 10 10.000 53.57 100.000 95 100.000 80-20.3000 27 1.000 &lt; 10 10.000 &lt; 10 100.000 71.98 28 1.000 &lt; 10 10.000 17.89 100.000 81.04 29 1.000 &lt; 10 (Please read the precautions on the back before filling out this page). Installation, ^ Γ. -407- (degrees apply to China_Country Standards (CNS) A4 specifications (210x297 public love) _ B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (4 06) Compounds Example number HIV protease FITC analysis HIV-1 dose (uM) ΗΠ- 1 Protease Inhibition% HIV-1 Protein Plum (uM) 10.000 54.17 100.000 98.44 30 1.000 &lt; 10 10.000 65.31 100.000 109.39 22 1.000 &lt; 10 10.000 &lt; 10 100.000 58.74 31 ι.οοα &lt; 10 10.000 &lt; 10 100.000 53.74 LOOO &lt; 10 10.000 &lt; 10 100.000 53.74 * 32 1.000 &lt; 10 10. 000 &lt; 10 100.000 46.45 33 1.000 &lt; 10 10.000 11.18 100.000 77.43 40 1.000 &lt; 10 10.000 &lt; 10 100.000 51.33 41 1.000 &lt; 10 10.000 32.57 100.000 80.63 42 1.000 11.46 10.000 75.2 100.000 112.15 100.000 102.8 9.9000 408- (Please first Read the notes on the back and then fill in the book.) This paper size applies to China National Standard (CNS) A4 specifications (210x297 mm). 5. Description of the invention (407) A6 B6 Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. FITC analysis of HIV compound protease examples | HIV-1 agent ft (uM) HIV-1 protein sea inhibitory HIV-1 protease 1 IC ^ iuM) 43 1.000 28.39 10.000 102.51 100.000 122.41 2.1000 25 1.000 11.44 10.000 78.63 100.000 115.12 5.2000 44 1.000 &lt; 10 10.000 &lt; 10 100.000 55.62 45 1.000 &lt; 10 10.000 28.46 _ 100.000 90.9 1 46 * 1.000 22.12… _ 10.000 96.29 100.000 Π6.4] 100.000 107 4.2000 47 1.000 &lt; 10 10.000 &lt; 10 100.000 `` 52- 95 23 I.Q00 46.62 10.000 96.62 0.6600 100.000 104.16 0.6 600 100.000 104.2 0.7000 48 1.000 &lt; 10 10.000 &lt; 10 ιοσοοο 43.3 24 1.000 &lt; 10 10-000 24.21 100.000 83.72 49 1.000 &lt; 10 • 4〇9— This paper size applies to China National Standard (CNS) A4 specifications ( 210x297 mm) ..................-............ ........... Φ ............ install ............... ....... Order ... J (Please read the notes on the back before filling out this page) A6 B6 V. Description of the invention (408) Ministry of Economic Affairs, Central Bureau of Standards, Consumer Cooperatives, printed compound examples, HIV protease HTC analysis, HIV-1 agent M (uM), HIV-1 protease inhibition% HIV-1 protein sea (uM) 10.000 21.93 100.000 60.32 50 1.000 33.5 10.000 80.29 100.000 95.54 23000 51 1.000 &lt; 10 10.000 &lt; 10 100.000 39.64 52 Ϊ.000 26.75 10.000 8L5 100.000 119.84 3.1000 53 1.000 &lt; 10 10.000 &lt; 10 100.000 71.84 54 1.000 &lt; 10 10.000 13.75 100.00 60.04 55 1.000 &lt; 10 10.000 &lt; 10 ιοο.όο ^ 7L98 56 1.000 &lt; 10 10.000 &lt; 10 * , 100.000 4952 57! .000 17.63 ιαοοο 94.39 100.000 99.32 2.8000 58 1-000 36.28 10.000 90.15 100.000 108.2 1.2000 59 1.000 &lt; 10 —410- (Please read the notes on the back before filling this page). Binding. Binding. Dimensions Applicable to China National Standard (CNS) A4 specification (210x ^ 97 gong) Printed by A6 B6, Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (408) Compound S Case No. HIV protein sea FITC analysis HIV- 1 (fi) HIV-1 protein sea inhibition% HIV-1 protease 丨 C $ 〇 (uM) 10.000 21.46 100.000 82.77 60 1.000 31.5 10.000 90.82 100.000 116.3 uooo 6! 1.000 77.83 1.0000 10.000 115.38 1.0000 100.000 Π9.04 1.0000 62 1.000 &lt; 10 10.000 10.56 100.000 78.3 63 L000 77.58 2.0000 10.000 90.32 2.0000 100.000 I1L31 2.0000 64 1.000 29.09 5.8000 10.000 78.09 5.8000 100.000 104 5.8000 39 1.000 13.79. 10.000 69J7 _ 100: 000 82.05 5.0000 | 76 1.000 &lt; 10 _ 10.000 47.8 100.000 96.48 77 1.000 &lt; 10 10.000 57.8 100.000 92.46 65 L000 & l t; 10 10.000 48.43 —_ 100.000 86.13 I 104 1.000 12.15 6.7400 -411- This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) (Please read the precautions on the back before filling this page)

A6 B6 V. Explanation of the invention (410) Example of compound printed by the Consumer Cooperative of Yinyang Standard Bureau, Ministry of Economic Affairs, HIV protease FITC analysis, HIV-1 agent, (uM) HIV-1 protein plum inhibition% HIV-1 protease (uM) 10.000 68.74 6.7400 100.000 105.84 6.7400 78 1.000 &lt; 10 8.4000 10.000 65.68 8.4000 100.000 83.55 8.4000 79 1.000 &lt; 10 13.1000 10.000 61.04 13.1000 100.000 80.86 13.1000 80 1.000 &lt; 10 8.5000 10.000 62.58 8J000 100.000 101.62 8J000 81 1.000 62 3.7000 10.000 70.000 75.6 85.3 3.7000 82 1.000 30.95 10.000 69.65 0.9000 100.000 88.% 0.9000 83 1.000 &lt; 10 _ U ........-- 10.000 &lt; 10 100.000 50.08 84 1.000 &lt; 10 I 10.000 30.2 85 1.000 &lt; 10 10.000 31.6 100.000 100 ^ 86 1.000 10.46 10.000 56.94 100.000 95.84 87 1.000 &lt; 10 10.000 20.6 -412- (Please read the precautions on the back before filling out this page) This paper size applies to China National Standard (CNS) A4 specification (21〇k297 (Public address) / A6 B6 V. Description of the invention (411) Member of the Ministry of Economic Affairs Order Standards Bureau Industrial and consumer cooperatives printed compounds Example number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protein plum inhibition% HIV-1 protein sea iCm (uM) 100.000 78.97 88 1.000 80.04 10.000 107.82 100.000 i 17.82 1.5200 1.560 49.9 1.570 41.7 12.500 89.2 12.500 80.8 100.000 92 1.6000 100.000 93.5 2.0000 89 1.000 &lt; 10 10.000 10.3 100.000 52.04 90 1.000 &lt; 10 10.000 29.67 100.000 89.16 91 1.000 &lt; 10 10.000 38.43… 100.000 94.41 — 100.000 71.61 1 92 1.000 &lt; 10 10.000 67.8 100.000 113.14 93 1.000 23.22 10.000 79.42 100.000 109.4 100.000 91.7 20.6000 94 1.000 &lt; 10 10.000 44.67 L 100.000 96.37 -413- (谙 Please read the notes on the back before filling this page)-Binding. This paper size applies Chinese National Standard (CNS ) A4 specifications (210x297 mm) A6 B6 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (412) Compound example number HIV protein sea FITC analysis HIV-1 agent Dong (uV〇HIV-1 protein sea Inhibition of% HIV-1 protein (uM) 100.000 82.45 95 1.000 &lt; 10 10.000 34.71 100.000 79.6 96 1.000 &lt; 10 • 10.000, &lt; 10 100.000 48.7 97 1.000 &lt; 10 10.000 29.87 100.000 78.24 98 1.000 &lt; 10 10.000 &lt; 10 100.000 74.47 99 1.000 &lt; 10 ·· 10.000 &lt; 10 100.000 43.29 100 1.000 &lt; 10 10.000 1232 100.000 53 1: 000 &lt; 10 10.000 &lt; 10 100.000. 40.3 101 1.000 &lt; 10 10.000 &lt; 10 100.000 39.21 102 L000 &lt; 10 10.000 24.02 100.000 78.8 100.000 75.63 π 103 1.000 &lt; 10 1 -414- (谙 Please read the precautions on the back before filling out this page) ®: -Binding, binding. This paper size is applicable to China National Standard (CNS) A4 specification (210 ' χ297 mm) A6 B6 V. Description of the invention (413) Compound example number HIV protease FITC analysis HIV-1 agent S (uM) HIV-1 protease inhibition% HIV-1 protease ICjo (uM) 10.000 25.67 100.000 80.89 1.000 &lt; 10 10.000 21.23 100.000 87.29 J00.000 73.35 104 1.000 12.15 6.7400 10.000 68.74 6.7400 100.000 105.84 6.7400 105 4.8800 3.8800 {谙 Read the precautions on the back before filling in this page}. Installed Printed by the Central Standardization Staff Consumer Cooperative of the Ministry of Economy

V. Explanation of the invention (414) Table III Compound Example No. CV-1 Cell Analytical Dose (U &amp;) Inhibition% 10 100.0 0.0 300.0 57.0 11 100.0 64.0 300.0 78.0 f Please read the precautions on the back before filling in this page). Binding. Binding. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs -416- This paper size applies to China National Standard (CNS) A4 specifications (210 ^ 297 mm) V. Description of invention (415) A6 B6 Ministry of Economic Affairs Standard Bureau employee consumer cooperative prints table IV Compound example number HIV protein Sea FITC analysis HIV-1 dose. (UM) HIV-1 protein _ Inhibition% HIV-1 FITC Kl (nM) 208 1.000 72.61 10.000 95.45 100.000 94.17 59 _ … 90 109 1.000 &lt; 10 10.000 71.89 100.000 91.96 1090 1! 0 1.000 16.91 10.000 73.82 100.000 99.89 410 11!! .000 36.48 10.000 94.33 100.000 100.65 700 丨 07 1.000 90.73 10.000 100.82 100.000 101.48 20 12 7 112 1.000 70.14 10.000 102.07 100.000 104.69 96 113 ι.οοο 39.58 {Please read the notes on the back before filling this page I. Installation -417- V. Description of the invention (416) A6 B6 Compound printed by the Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Example number HIV protease FITC analysis HIV-1 agent S (uM) HIV-1 protease inhibition% HIV -1 FITC ΚΙ (nM) 10.000 99.82 100.000 109.29 114 1.000 &lt; 10 10.000 &lt; 10 100.000 14.13 115 1.000 62.1 10.000 102.46 100.000 129.37 177 116 1.000 22.97 10.000 65.66 100.000 102.31 558 118 0.410 68.66 1.230 87.89 3.700 98.96 11.000 109.98 39.9 105.25 57 117 0.410 80.14 1.230 93.99 3.700 101.36 11.000 113.61. 33.000 107.44 100.000 99.97 37 119 0.410 27.46 1: 230 55.43 3.700 82.46 1 (Please read the precautions on the back before filling this page). Binding, 418- 'This paper size Applicable to China National Standard (CNS) A'4 specification (210 × 297 mm) V. Description of the invention (417) A6 B6 Printed paper compound printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs, Case No. HIV protein, FITC analysis of HIV -1 dose suspension (uM) Hiv-i protein feet Inhibition% HIV-1 FITC Kl (nM) 11.000 97.65 33.000 96.76 100.000 101.38 257 122 0.410 35-13 1.230 63.53 3.700 91.69 11.000 98.01 33.000 93.25 100.000 94.27 175 123 0.410 23.71 1.230 59.06 3.700 82.49 11.000 88.31 33.000 83.92 10 0.4 78.91 lt. ; 10 1.230 32.42 3.700 65.59 Π.000 81.63 33.000 S8.16 100.000 89.39 1035 125 0.410 10052 1.230 107.7 3.700 107.85 11.000 108.48 33.000 1Q2J27 (Please read the notes on the back before filling out this page} Binding: -419- A6 B6 Ministry of Economy Printed by the Central Consumer Bureau of Consumer Standards Co., Ltd. 5. Description of the invention (418) Compound example number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protein sleep inhibition% HIV-I FITC KI (nM) 100.000 105.34 24 120 0.410 &lt; 10 1.230 22.2 3.700 54.63 11,000 80.69 33.000 10UI 100.000 105.81 982 126 0.410 25.86 1.230 59.05 3.700 89.8 11.000 96.66 33.000 100.02 100.000 95.04 331 135 0.410 87.06 1.230 92.51 3.700 96.65 11.000 82.44 33.000 71.16 100.000 63.63 30 121 0.123 37.il 0.370 74.9 1.100 99.53 3.300 106-16 10.000 107.79 30.000 108.63 24 (Please read the precautions on the back before filling out this page) -Installation · OK. -420— This paper is a j-size national standard (CNS) A4 specification (210x297 public love) A6 B6 V. Description of invention (419) Example number of compound printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Η Protease FITC analysis HIV-1 Agent S (uM)% HIV-1 protease inhibition HIV-I F1TC KI (nM) 127 0.123 52.32 0.370 92.55 1.100 111.91 3.300 115.12 10.000 117.38 30.000 111.35 33 128 0.123 32.5 0.370 85.6 1.100 101.62 1300 112.49 10.000 107.42 30.000 102.3 26 1 ^ 9 0.123 23J9 0.370 WJ9 1.100 96.53 3.300 106.34 10.000 U6.53, 30.000 120.4 31 130 0.123 &lt; 10 0.370 14.73 1.100 54 3.300 88.61 ιο.ΰόο 103.93 30.000 112 119 134 0.123 &gt; 54.05 0.370 97.73 -421- {Please read the back first Note: Please fill in this page again) Binding, binding, paper ruler, and watts are in accordance with China National Standard (CNS) A4 specification (210x297 mm) A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 420) Compound example number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protein sea inhibition% HXV-1 FITC KI (nM) 1.100 103.67 3.300 110 ^ 4 10.000 i 10.97 30.000 109.35 15 131 0.123 30.73 0.370 74.24 1 100 98.71 3.300 ili.87 10.000 116.04 30.000 105.99 30 132 0.123 &lt; 10 0.370 39.51 1 "00 76.22 3.300 98.14 10.000 104 * 27 30.000 102.65 _ +,-50 133 0.123 19.06 0.370 71.18 1.100 97.94 3.300 100.79 10.000 10L2 30.000 99.48 12 i4l 1.000 14.21 10.000 77.37 100.000 102.75 142 1.000 &lt; 10 -422- (Please read the notes on the back before filling out this page). Binding ·-This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) A6 B6 Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs 421) Compound reward number HIV protease FITC analysis HIV-1 SHS (uM) HIV-1 protease inhibition% HIV-1 FITC KI (nM) 10.000 15.65 100.000 71.77 143 1.000 10.79 10.000 77.11 100.000 92.12 144 1.000 25.95 10.000 77.03 100.000 85.99 145 1.000 37.01 10.000 81.05 100.000 97.05 146 1.000 54.41 10.000 92.66-100.000 98.64 130 147 1.000 34.67 10.000 86.35 100.000 96J3 148 1.000 &lt; 10 10.000 57.85 100.000 93.69 149 1.000 28.83 10.000 99.21 100.000 97.27 405 150 L (XX) &44; 10 10.000 100.000 93.01 151 1.000 29.13 10.000 82.85 1 -423 · (Please read the precautions on the back before filling out this page) ·-. Binding and binding. This paper size applies to China National Standard (CNS) A4 (210x297 Gongcheng) A6 B6 Printed by a member of the Central Standards Bureau of the Ministry of Economic Affairs and printed by a consumer cooperative. 5. Description of the invention (422) Examples of compounds Tweezers HIV protein sea HTC analysis HIV-1 agent S (uM) HIV-1 protease inhibition% HIV-I FITC KI (nM) 100.000 92.38 152 0.410 &lt; 10 L230 14.2 3.7 00 35.52 11.000 73.68 33.000 102.03 100.000 109.77 2012 138 1.000 11.89 10.000 64.54 100.000 99.32 2350 | 137 1.000 11.27 10.000 62.92 100.000 89.08 1750 2200 154 1.000 13.63 10.000 77.13 100.000% .05 丨 '520 155 1.000 15.41 10.000 74.9 .- 100.000 91. 17.13 10.000 33.56 100.000 63.72 139 1.000 36 ^ 6 — 10.000 80.73 100.000 99.15 —424— 'Tai Paper Paper Boats ♦ Group S! · Jinhuanbao ^ ΓΜβ, Tian mnw〇nrr, \ * · _, {Please read first Note on the back, please fill out this page) f! R 5 丁-¢-

I. Explanation of the invention (423) A6 B6 Ministry of Economic Affairs t Central Standards Bureau Employees Cooperative Co-operative Compounds Printed Compound Reward Number HIV Protease FITC Analysis HIV-1 Dose (uM) HIV-1 Protease Inhibition% HIV-1 FITC KI (nM ) 500 157 1.000 &lt; 10 10.000 &lt; 10 100.000 63.99 158 1.000 &lt; 10 10.000 26.73 100.000 93.38 140 0.410 &lt; 10 1.230 16.49 — 3.700 48.12 11.000 71.76 33.000 91.07 100.000 108.87 762 159 0.410 &lt; 10 1.230 14.39 3.700 39.76 11.000 74.27. 33.000 84.24 100.000 91.14 2397 160 0.410 &lt; 10 1.230 &lt; 10 3.700 &lt; 10 11.000 14.21 _ .........--... 33.000 40.35 100.000 82.56 161 32 162 40 | 163 34 -425- This paper ruler is used for group tour (f! NS) Tian A is / 91 Γϊ * «_,-/ u (Please read the precautions on the back before filling this page) ... &quot; A6 B6 V. Description of the invention (424) Example of compounds printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs Example # HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protein sea inhibition % HIV-1 FTTC KI (nM) 316 0.123 10 0-370 31.24 1.100 77.76 3.300 98.14 10.000 102 * 56 30.000 110.55 18 317 0.123 27.78 0.370 46.7 1.100 81.71 3.300 10L3 10.000 102.05 30.000 112.86 11 318 0.123 28.3 0.370 45.08 U00 84.18. 3.300 99.67 10.000 91S1 30.000 105.81 9.9 363 0.123 10 0.370 10 U00 21J1 3.300 58.75 —....... 10.000 84.82 30.000 107.37 364 0.123 10 0.370 17.22 1.100 53.5 3.300 78.67 10.000 100.25 30.000 90.21 118 (Please read the precautions on the back first (Filling page). Packing • ΤΓ. ¥ This paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) V. Description of invention (425) A6B6 Member of the Central Standards Bureau of the Ministry of Economic Affairs 钃 Examples of compounds printed by consumer cooperatives 钃No. II protease FITC analysis HIV-1 dose (uM) HIV-1 protease inhibition% HIV-1 FITC K1 (nM) 365 0.123 11.74 0.370 31.05 1.100 65.28 3.300 84.07 10.000 94.54 30.000 95.78 63 319 0.123 67.05 0.370 84.24 1.100 93.13 3.300 94.29 10.000 101.95 30.000 101.42 4.3 3.3 2.1 320 0.123 66.37 0.370 78.55 L100 98.19 3.300 102.32 10.000 99.29 30.000 99.03 3.8 2.1 321 0.123 22J2 0.370 62.06 1.100 100.03 3.300 113.11 10.000 118.85 30.000 117.97 13.2 322 0.123 10 0.370 10 (100 22.31 -427 Read the notes on the back before filling out this page}. Binding. ¥?-Ϊ-

I. Description of the invention (426) Example number of gas-producing compounds in the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs HIV protease FITC analysis HIV-1 dose (uM) Hiv-i protease / inhibition% HIV-1 FITC KI (nM) 3.300 61.14 10.000 91.75 30.000 105.97 323 0.123 62.79 0.370 91.81 1.100 100.2 3.30 104.32 10.000 118.05 30.000 112.33 6.3 324 0.123 44.33 0.370 87.46 1.100 103.02 3.300 10823 10.000 115.62 30.000 117.15 4.0 325 0.123 59.78 0.370 86.58 1.100 95.56 1.300 1 385 3.97 105.1 1 38 0.123 51.64 0.370 92.56 1.100 10L5 3.300 105.93 10.000 114.14 30.000 121.02 4.600 (Please read the precautions on the back before filling this page) • »428—

A6 B6 V. Explanation of the invention (42) Compound example number HIV protease FITC analysis HIV-1 protease inhibition% HIV-1 FTTC KI (nM) 327 0.123 34.22 0.370 68.19 1.100 94.75 3J00 105.37 10.000 105.72 30.000 112.78, 13.5 264 0.123 78.52 0.370 89.02 U00 99.82 3.300 104.42 10.000 108.11 30.000 108.96 2.5 265 0.123 25.34 0.370 54.77 U00 76.87 3.300 86.12 10.000 100.44 30.000 98.35 31.5 244 〇, 121 10 0.370 10 1.100 10 3-300 10 10.000 18.84 30.000 31.78 266 0.123 79.8 1.100 0.370 88. 10U9 3.300 100.36 10.000 104.64 1 -429- L degrees (using China National Standard (CNS) A4 specifications (210X297 mm)

A6 B6 V. Description of the invention (4 Hung) Example of compound printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Example # HIV protein South PITC analysis HIV-1 agent fi (uM) HIV-1 protein _ Inhibition% HIV-1 FTTC KI ( oM) 30.000 102.86 4.1 267 0.123 71.48 0.370 83.88 1.100 92.02 3.300 107.29 10.000 106.97 30.000 109.94 / 6.2 269-0.123 77.14 0.370 95.65 1.100 1Π.83 3.300 11429 10.000 124.96 30.000 114.06 2.9 270 0.123 61 67 0.370 93.12 1.100 107 * 2 3.300 0 * 59 10.000 115.96 30.000 114.73 5J 258 7.6 401 2.3 257 3.0 261 3.1 268 0.123 71.24 0.370 88 1.100 96.15 3.300 97.62 10.000 101.31 30.000 101.17 3.1 • 430- (Please read the precautions on the back before filling this page} '装 • ΤΓ . j applicable + national time standard (GNSW specification (210x297 mm) 5. Description of invention (429)

Compound Example No. HIV Protease FITC Analysis HIV-1 Dose (uM) HIV-1 Protease Inhibition% HIV-1 FITC Kl (nM) 271 0.123 10 0.370 16.69 1.100 47.45 3.300 75.32 10.000 88.81 30.000 94.23 74.3 272 0.123 67.1 0.370 85.25 1.100 95.35 3.300 96.23 10.000 100.68 30.000 104.08 2.1 273 0.123 68.41 0.370 92.26 1.100 95.9 3.300 98.15 10.000 101.66 30.000 108.32 2.7 274 0.123 70 0.370 88.17 1.100 95.85 3.300 98.83 10.000 102.79 30.000 105.14 4.7 275 0.123 79.26 0.370 120.000 3.0.00 1 00 1.27 1. -431- The size of this paper is in accordance with the national standards of the ten countries. A4 size (210x297 male dragon_) V. Description of the invention (430) A6 B6 Example of compound printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. HIV-1 agent (uM) HIV-1 protein sea inhibition% HIV-1 RTC KI (nM) 276 0.123 53.36 0.370 92.75 1.100 99,28 3.300 94.72 10.000 112.32 30.000 123.9 11 277 0.123 10 0.370 10 1.100 10 3.300 37.89 10.000 79.93 30.000 94.12 278 0.123 36.28 0.370 78.17 '1: 100 94.73 3.300 10056 10.000 101.68 30.000 1103 13.6 280 0.123 69.76 0.370 95.1 U00 10054 3.300 109 ^ 5 10.000 109.82 30.000 1133 5 279 0.123 78.2 0.370 97.29 1.100 105.27 3.10 108.88 30.000 94.85 4.1 -432 · The paper ruler Yanjin uses the life group® to set up the following 卩 rws) Tian Gu, Of Λ k, f one * 3 free (please read the precautions on the back before filling this page) -pack- Order A6 B6 V. Description of the invention (431) Ministry of Economic Affairs t Central Standards Bureau Employees' Cooperatives Printed Compounds Example Number HIV Protein Sea FITC Analysis HIV-1 Dose (uM) HIV-1 Protease Inhibition% HIV * I FTTC KI (nM ) 281 0.123 5551 0.370 93.52 1.100 99.3 3.300 109.39 10.000 105.4 30.000 101.02 10.6 328 0.123 11.95 0.370 45.95 U00 86.57 3.300 105.92 10.000 113.94 30.000 111.06 33 329 0.123 10 0.370 10.17 1: 100 42.19 3.300 75.33 10.000 91.77 30.000 10IJ2 330 75 U00 105.73 3.300 108.94 10.000 114.61 30.000 106.38 9.3 331 0.123 66.39 0.370 86.S9 V. 1.100 99.22 3.300 118.95 10.000 121.29 30.000 105.29 4.8 -433 * (Please read the precautions on the back before filling this page). Binding. This paper size Applicable to National Standards (CNS) A4 niobium (210x297 mm) V. Description of the invention (432) A6 B6 Compounds printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Case number HIV protein Sea FITC analysis HIV-1 (UM) HIV-1 protease inhibition% HIV-1 FITC KI (ηΜ) 262 0.123 83.32 0.370 102.6 U00 112.99 3.300 121.87 10,000 119 * 5 1 30.000 114 ^ 4 1.4 0.44 1.01 0.6 0.6 332 0.123 23.14 0.370 39.26 1.100. 71.55 3.300 93.95 10.000 108J6 30.000 114.97 47 333 0.123 10 0.370 28.33 1.100 62.17 3.300 82.05 10.000 101.66 30.000 i 10.31 104 246 0.123 10 0.370 10 1.100 10 3.300 10 10.000 26.64 30.000 49.66 245 0.123 10 0.370 10 (Please read the notes on the back and fill in the book Page} Binding V. -434 ^. I Degree Applicable National Standard (CNS) A4 Specification (210x297 Public Love) A6 B6 V. Description of Invention (433) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs

Example of compound FITC analysis of HIV protease HIV-1 agent 1 (UM) HIV-1 protein sea inhibition% HIV-1 FITC K1 (nM) 1.100 10.64 3.300 50.92 10.000 59.51 30.000 78.63 408 0.123 37.1 0.370 69.39 1.100 87.61 3.300 85.17 10.000 97.39 30.000 97.21 18.1 283 0.123 10 0.370 10.6 L100 42.27 3.300 64.22 10.000 85.12 30.000 80.21 284 0.123 37.48 0.370 77.05 LI00 99.82 3.300, 106.85 10.000 106.87 30.000 10428 12.2 285 0.123 37.64 0.370 73.79 1.100 84.61 3.30O 95.04 0.10.000 97.66 10.000 97.66 10.000 97.66 10.000 97.66 10.000 62.4 _: I -435- (Please read the precautions on the back before filling this page) Binding. Binding. 4. This paper size is applicable to National Standard (CNS) A4 specifications (210X297 mm) 5. Description of the invention (434) A6 B6 Compounds printed by employees' cooperatives of the Xinyang Standard Bureau of the Ministry of Economics Example number HIV protein Sea FITC analysis HlV-lSJfi (uM) HIV-1 protease inhibition% HIV-l FITC KI (nM) 1.100 83.35 3.300 92.28 10.000 97.44 30.000 93.69 21.4 287 0. 123 IO 0.370 14.06 1.100 44.1 3.300 68.19 10.000 85.78 30.000 86.72 263 0.123 82.88 0.370 89.92 1.100 95.73 3.300 98.67 10.000 107.98 30.000 98.33 1.9 334 0.123 10 0.370 13.61 UOO 42.28 3.300 69.04 10.000 87.61. 30.000 89.51. 0.370 0.373 0.133 10.000 96.48 30.000 105.84 6.8 336 0.123 73.53 0.370 87.27 —436— (Please read the notes on the back before filling this page). Binding. -Line.

V. Description of the invention U35) A6 B6 Compound number printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Example number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protease inhibition% HIV-I FTTC KI (nM) 1.100 92.95 3.300 94.63 10.000 103.23 30.000 108.08 5,3 337 0.123 10.11 0.370 47.88 1.100 93.62 3.300 116.43 10.000 110.8 30.000 111.88 37.9 338 0.123 39.07 0.370 80.12 1.100 86.33 3.300 96.8 10.000 101.65 30.000 99.96 9,8 339 0.123 53.55 0.370 81.33 1.100 94.89. 99.300 3.99 3.300 7A I 340 0.123 77.79 L .....— 0.370 93.2 1.100 90.86 3.300 96.54 1Q.000 100.53 30.000 96.54 1.9 | 288 0.123 46.91 1 0.370 79.06 (Please read the precautions on the back before filling this page) Mang · 1 ^ ε Binding-binding-line; -437- This paper size applies to the National Standard (GNS) ^ 4 size (210x297 mm) A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (436) 11 '(: Analysis of HIV-1 Dose (uM) HIV-1 White enzyme inhibition% HIV-I FITC KI (αΜ) 1.100 90.47 3.300 92.86 10.000 105.45 30.000 101.46 6.9 289 0.123 63.71 0.370 80.05 1.100 91.12 3.300 97.3 10.000 95.28 30.000 100.75 2.7 290 0.123 90.26 0.370 H5.I2 1.100 123.27 &amp; 1.300 125.99.119.99. 30.000 114.37 2.7 291 0.123 80.41 0.370 108.02 1.100 109.27 3.300 121.93 10.000 117.89 30.000 116 ^ 5 2.6 292 0.123 74,42 — 0.370 103.91 1.100 111.33 3.3—00 124.78 10.000 115.11 30.000 111.07 4.5 I 293 0.123 54.91 1 0.370 82.42 _1 -438- Please read the notes on the back before filling in this page)-Binding. Staple: This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) A6 B6 V. Description of invention (43) Central standard of Ministry of Economic Affairs Examples of compounds printed by the Bureau ’s Consumer Cooperatives. No. HIV protease FITC analysis HIV-1 agent (uM) HIV-1 protease inhibition% HIV-1 FITC KI (nM) U00 96/83 3.300 107.39 10.000 10538 30.000 108.57 9.3 295 0.123 10 0.370 10 1.100 25.9 3.300 57.05 10.000 87.53 30.000 100.17 409 0.123 10 0.370 20.9 1.100 52.87 3.300 81.06 10000 94.6: 30.000 110.5 139 251 1 * 25 250 1.23 259 0.71 255 0.62 296 0.123 14.62 0.370 74.77 uoo 95.51 3.300 10334 10.000 107.8 30.000 114.11 24 0.3297 0.123 86.01 1.100 10052 3.300 99.81 (Please read the precautions on the back before filling this page) _ Installation-line _ This paper size adopts China National Standard (CNS) f 4 specifications (210x297 mm) 5. Explanation of the invention (438) Economy Printed by the Consumer Standards Cooperative of the Ministry of Standards

Example of compound FITC analysis of HIV protease | HIV-1 HIV-1 (uM)% HIV-1 protease inhibition HIV-1 FITC | ΚΙ (nM) 10.000 101.63 30.000 99.54 1.6 298 0-123 67.39 0.370 84.64 L100 94.6 3.300 97.5 10.000 100.9 30,000 100 2.5 299 0.123 78.54 0.370 97.78 1.100 97.46 3.300 91.67 10.000 104.35 30.000 98.38 2.3 300 0.ι23 68.8 0.370 92.23 1.100 100.71 3.300 101.51 10.000 108J5 3〇.οοα 108.43 3.1 301 0.123 74.65 0.370 91.19 UOO 10152 3.300 100.41 0.00 10.000 302 0.123 78.61 0.370 97.82 1.100 104.55 I 3.300 Π235 1 • 44 * 0—one piece of paper and one copy of paper. Degrees apply to S family standards⑽S) A__ Specifications (21GX297 public love) A6 B6 V. Invention Description (439) Economy Ministry of Central Standards Bureau, Consumer Cooperatives, printed compound examples, HIV protease FITC analysis, HIV-1 dose (uM), HIV-1 protein sea inhibition% HIV-1 FITC KI (nM) 10.000 115: 31 30.000 112.47 2.7 303 0.123 67.38 0.370 96.54 1.100 97.65 3.300 109.02 10.0 00 109.9 30.000 97.99 5 304 0.123 25.71 0.370 60.19 L100 85.93 3.300 97.82 10.000 1030 30.000 95.57 27,9 34; 0.123 59.43 0.370 92.77 1.100 109-68 3.300 107.4 10.000 120.47 30.000 122.42 5 342 0.123 42.05 0.370 72.88 U00 88.22 3.300 97.97. 〇.οώ 104.99 10.9 343 0.123 39.4 0.370 74.98 1.100 91.21 3.300 104.19 {Please read the precautions on the back before filling out this page} -yl Meaning, binding, ordering. -Line · This paper size applies to Chinese National Standard (CNS) A4 Specifications (210x297 mm) A6 B6 V. Description of the invention (44) The compound number printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economics Example number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protein sea inhibition% HIV- 1 FTTC KI (nM) 10.000 111.99 30.000 105.32 6 344 0.123 10 0.370 10 1.100 11.78 3.300 32.69 10.000 63.21 30.000 81.83 410 0.123 60.37 0.370 86.24 1.100 92.37 3.300 95.2 10.000 99.81 30.000 106 * 54 6.2 306 0.123 10 0.370 10 1.100 24.42 3.42 3. 300 53.25 10.000 74.49 30.000 86.22 308 0.123 46.49 0.370 70.42 1.100 82.28 3.300 91.26 10.000 96.86 30.000 86.75 31 309 0.123 46.56 0.370 67.45 U00 82.49 3.300 76.55 ............... 442 Please read the note on the back first Please fill in this page again for this matter) This paper size is applicable to the Tans Standard (CNS) f 4 specification (210x297 public dream)

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V. Description of the invention (441 J Compounds printed by employees of the Central Standards Bureau, Ministry of Economic Affairs, Consumer Cooperatives, Compound No. HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protease inhibition% HIV-1 FITC ΚΙ (αΜ) • 10.000 43.74 30.000 19.22 5.8 254 0.123 49.54 0.370 79.73 1.100 91.4 • 3300 90.9 10.000 96.84 30.000 98.32 8.8 253 0.123 69.79 0.370 86.65 1.100 84.79 3.300 91.63 10.000 97.46 30.000 101.45 1.7 2.4 252 0.123 100.07 0.370 107.91 1.100 110J7 3.300 111.98 18.6 98 1 0.123 50.05 0.370 77 1.100 90.39 3.300 10056 10.000 104.61 30.000 91.85 13.1 346 0.123 75.09 0.370 915 -443- (Please read the notes on the back before filling out this page). Binding?-Λ V. Invention Description (442) A6 B6 Ministry of Economy Printed by the Central Bureau of Standards Consumer Cooperatives-Compound Example No. HIV Protease FITC Analysis HIV-1 ul fi (uM) HIV-1 Protease Inhibition% HIV-1 FITC KI (nM) 1.100 97:31 3.300 102.38 10.000 102.7 30.000 97 3.85 347 0.123 79.84 0.370 92.19 1.100 103.43 3.300 100.21 10.000 102.08 30.000 102.85 2J 314 0.123 79.52 0.370 97.7 1.100 107.73 3.300 109.14 10.000 102.22 30.000 97.14 2.31 2.01 260 0.123 73.79 0.370 91.66 1.100 98.97 3.300 106.23 10.000 1.86 102.36 0.90 102.36 102.36 0 3.300 95.02 10.000 101.04 30.000 96.12 0.42 307 0.123 19.57. (Please read the notes on the back before filling out this page) A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (443) Compound instance number HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protease inhibits HIV-FITC K1 (nM) 0.370 66.55 1.100 85.23 3.300 97.75 10.000 104.73 30.000 90.27 7.6 349 0.123 10 0.370 38.43 1.100 69.0! 3.300 86.41 10.000 96.72 30.000 88.45 33.8 310 0.123 46.21 0.370 86.18 1.100 94.87 3.300 99.05 10.000 102.79 30.000 102.21 2.37 311 0.123 20.75 0.370 71.24 1.100 86 .43 3300 91.96 10.000 99.54 30.000 99.48 6.33 348 0.123 28.13 0.370 80.67 1.100 102.66 3.300 108.46 10.000 113.04 30.000 108.91 6.9 348 0.123 38.62 (Please read the precautions on the back before filling out this page) Packing -445- The size of this paper is suitable for the country Painter's standard (CNS) A4 specifications (210x297 mm) V. Description of invention (444) A6 B6 Printed compounds by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs Example compound number HIV protein Sea FITC analysis HIV-1 dose 〇ιΜ) HIV -1 Protease Inhibition% HIV-I FTTC ΚΚπΜ) 0.370 81.05 1.100 102.34 3.300 108 * 55 10.000 112.78 30.000 98.7 1.7 403 0.123 49.67 0.370 78.53 1.100 97.9 3.300 104J 10.000 101.85 30.000 94J9 2.S4 353 0.123 48.58 0.370 83.12 1.100 92.65 3.300 97.300 102.6 30.000 92.88 2.25 312 0.123 48-17 0.370 83.6 1.100 89.74 3.300 106.17 10.000 114 30.000 109.93 4 404 0.123 4K64 0.370 77.47 1.100 92.92 3.300 94.76 10.000 95.57 30.000 97.01 5 405 0.123 83.76 (please first Read the notes on the back and fill in this page again) -Installation—446— This paper size applies to the ten national standards (CNS) A4 specifications (210x297 mm) V. Description of the invention (445) A6 B6 Staff consumption of the Central Standards Bureau of the Ministry of Economic Affairs Printed by Cooperative Society-.f Compound Example # No. II Protease FITC Analysis HIV-lSIfi (uM) HIV-1 Protease Inhibition% rav-i fitc KI (nM) 0.370 105 * 53 1.100 114.88 3.300 115.96 10.000 116.92 30.000 116.11 1.86 254 0.123 82.28 0.370 97.98 1.100 丨 07.75 3.300 i 11.05 10.000 112.1 30.000 103.1 0.65 406 0.123 58.26 0.370 85.28 1.100 102.83 3.300 108.5 10.000 105 ^ 30.000 102.67 2.87 161 0.123 20.02 0.370 67.29 1.100 98.69 3.300 103.91 10.000 106.32 30.000 111.13 32.162 1.23 0.323 1.81 14.23 99.34 10.000 101J7 30.000 108.88 40 163 0.123 17.66 -447- {Please read the notes on the back before filling this page) Binding. Ir * * 1¾. Γ5. 4 &lt; 0 **-A6 B6 V. Description of the invention (446) Staff Consumption of Central Bureau of Standards, Ministry of Economic Affairs Examples of compounds printed by Sakusha Co., Ltd. HIV protease FITC analysis HIV-1 agent (uM) HIV-1 protein sea inhibition% HIV-I FITC KI (nM) 0.370 55 ^ 5 1.100 84.23 3.300 98.56 10.000 107.38 30.000 104.74 34 170 0.123 23.25 0.370 62.26 1.100 92.5 3.300 99.3 10.000 107.29 30.000 110.83 31 171 0.123 33.13 0.370 73.44 U00 96.52 3.300 103.16 10.000 109.98 30.000 108.64 23 172 0.123 &lt; 10 0.370 &lt; 10 L100 31.92 3.300 73.45 10.000 97.83 30.000 109.61; 173 0.123 10 U00 15.01 3.300 36.54 10.000 76.69 30.000 97.16 174 0.123 11.38 (Please read the notes on the back before filling out this page)-Binding. Staple. This paper size applies to China National Standard (CNS) A4 specifications (210x297 mm) V. Description of the Invention (447) Compound Example Number HIV Protease FITC Analysis | HIV-1 Dose (uM) HIV-1 Protein Sea Inhibition% HIV-1 FITC KI (nM). 0.370 35.75 1.100 75.02 3.300 95.89 10.000 104.18 30.000 97.78 35.000 I 175 0.123 &lt; 10 0.370 &lt; 10 1 .100 19.41 3.300 55.47 10.000 88.54 30.000 104.57 176 0.123 &lt; 10 0.370 27.32 U00 82.58 3.300 104.01 10.000 109.26 30.000 117.62 37.000 177 0.123 &lt; 10 0.370 16.86 1.100 53.85 3.300 88.93 10.000 103.65 30.000 104.3 55.000 1.98 1.44 16.24 16.23 16.24 10.000 104.94 I 30.000 102.6 27.000 | 179 0.123 &lt; 10 1 —449— A6 B6 V. Description of the invention (448) Example number of the compound printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. (uM)% HIV-1 protease inhibition HIV-I FITC KI (nM) 0.370 38.65 1.100 71.63 3.300 87.25 10.000 93.69 30.000 91.08 19.000 180 0.123 &lt; 10 0.370 &lt; 10 1-100 31.3 3.300 67.67 10.000 94.14 30.000 109.37 181 0.123 &lt; 10 0.370 &lt; 10 L100 10.44 3.300 35.1 10.000 66.6 30.000 79.26 182 0.123 &lt; 10 0.370 22.26 1.100 51.02 3.300 83.72 10.000 99.18 30.000 98.67 117.000 183 0.123 20.92 0.370 56.5 1.100 85.54 3.300 97.33 10.000 95.76 30.000 89.71 13.000 | 184 0.123 &lt; 10 1 -450- (Please read the precautions on the back before filling out this page)-Binding. Paper ruler. Use national standards (CNS) A4 specifications (210x297 public love) V. Description of the invention (449) A6 B6 The compound number of the compound printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs, from protease? 11 (: Analysis of HIV-1 agent fi (uM) HIV-1 protein sea inhibition% HIV-1 FITC KI (nM) 0.370 18.Ό4 1.100 60.74 3.300 85.97 10.000 96.51 30.000 93.08 46.000 185 0.123 18.73 0.370 40.26 1.100 71.53 3.300 92.59 10.000 97.64 30.000 91.75 22.000 186 0.123 &lt; 10 0.370 &lt; 10 1.100 29.2 1300 64.59 10.000 88.74 30.000 100.99 187 0.123 &lt; 10 0.370 10.6 1.100 32.87 3.300 67.96 10.000 89.99 30.000 90.15 188 0.123 27.26 uoo 82.16 0.370 57.02 3.300 88.4 10.000 88.46 189 0.123 15.66 {Please read the precautions on the back before filling this page}. Installation, ΤΓ. -V. -451- This paper applies the Chinese National Standard (CNS) A4 specification (21QX297 mm). 5. Description of the invention ( 45〇) A6 B6 Compounds printed by the Consumer Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs, Example No. HIV protease FITC analysis HIV-1 dose (uM) HIV-1 protease inhibition% HIV-1 FITC ΚΙ (ηΜ) 0.370 37.62 U00 69.77 1300 89.35 10.000 98.11 30.000 9935 36.000 190 0.123 &lt; 10 0.370 &lt; 10 U00 35.86 3.300 79.27 10.000 96 30.000 HXL5 191 '0.123 &lt; 10 0.370 16.94 1.100 54.96 3.300 93.35 10.000 100.92 30.000 100.04 192 0.123 &lt; 10 0.370 &lt; 10 1.100 24.9 3.300 68.77 10.000 10231 30.000 102.35 193 0.123 &lt; 10 0.370 &lt; 10 U00 35.01 3.300 70.38 10.000 97.73 30.000 105.39 194 0.123 &lt; 10 -452- (Please read the precautions on the back before writing this page}. Binding. Ordering-ti Γ 15. Explanation (451) A6 B6 A member of the Central Standards Bureau of the Ministry of Economic Affairs, a compound printed by a consumer cooperative «Examples of HIV protease FITC analysis HIV-1 agent (uM) HIV-1 protein _ Inhibition% HIV-1 FITC ΚΙ (nM) 0.370 39.7 , 1.100 81.89 3.300 102.84 10.000 108.17 30.000 107.45 28.000 195 0.123 &lt; 10 0.370 23.47 1.100 71.37 3.300 90.85 10.000 108.07 30.000 11726 22.000 196 0.123 67.96 0.370 812 U00 91.83 3.300 97.93 10.000 104.68 30.000 95.75 3.100 197 61.3 0.398 33.98 0.361. .300 88.68 10.000 91.75 30.000 89.62 14.100 198 0.123 67.11 0.370 91.89 U00 107.19 3.300 111.11 10.000 114.95 30.000 115.88 6.900 199 0.123 55.99 (Please read the precautions on the back before filling out this page). Binding. Binding. -453- This paper size applies National halogen cable: Standard (CNS) A4 specification (210X297 mm) A6 B6 V. Description of invention (452) Compounds printed by employees' cooperatives of the Central Bureau of Standards of the Ministry of Economics Example number HIV protease FITC analysis Π-1 Dose suspension ( uM) HIV-1 protein_ Inhibition% HIV-1 FITC Kl (nM) 0.370 86.55 1.100 97.62 3.300 106.12 10.000 114.48 30.000 106.98 10.400 200 0.123 64.6 0.370 88.48 1.100 90.89 3.300 103.22 10.000 105.15 30.000 99.1 1900 201 0.123 31.16 0.370 60.1 t.iOO 80 3.300 95.36 10.000 100.21 30.000 107.07 13.900 202 0.123 20 &quot; 0.370 48.13 1.100 73.14. 3.300 88J2 — 10.000 93-82 _ 30.000 94J6 43.000 1 203 0.123 15.63 0.370 55.8 1.10Θ 81.33 3.300 94.35 10.000 104.01 30.000 94.35 31.800 1 204 0.123 49 -454- {谙 Read the precautions on the back first and then the page on Swallow Nest). Binding, V. This paper size applies the national standard (CNS) f 4 specifications (210X297 mm). V. Invention Note (453) A6 B6 Compounds printed by employees of the Central Standards Bureau, Ministry of Economic Affairs, Consumer Cooperative Co., Ltd. Example number HIV protein FTTC analysis HIV-1 dose (uM) HIV-1 protease inhibition% HIV-Ϊ FITC ΚΙ (αΜ) 0.370 ^ 86.53 1.100 106.92 3.300 114.18 10.000 116.83 30.000 116.04 11.000 205 0.123 12.58. 0.370 56.41 U00 76.57 3300 94.18 10.000 109.32 30.000 103.94 26.100 206 0.123 &lt; 10 0.370 17.93 1.100 48.05 3.300 &gt; 76.43 10.000 95.84 30.000 93.11.207.81 0.181 13.03 13.96 13.03 10.000 83.02 30.000 78.74 33.400 208 0.123 &lt; 10 0.370 &lt; 10 uoo 22.94 3.300 57.62 '10.000 76.76 30.000 81.4 209 0.123 &lt; 10 (Please read the notes on the back before filling out this page} #: Binding-booking. -455- This paper size applies to China National Standard (CNS) A4 specification (210X2 97 mm) A6 B6 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the Invention (454) Example of Compounds Articles HIV Protease FITC Analysis HIV-1 Agent Dong (uM) HIV-1 Protease Inhibition% HIV-1 FITC KI (nM) 0.370 43.24 1.100 79.98 3.300 96.02 10.000 104J21 30.000 100.09 24.100 210 0.123 19.67 0.370 31.46 1.100 58.11 3.300 77.58 10.000 88.76 30.000 97.28 55.000 211 0.123 &lt; 10 0.370 37.24 1,100 64.49 3.300 89.56 10.000 101.21 3.0.00 100. 94.45 3.300 102.35 10.000 1 (39.03 30.000 99.28 3J00 214 0.123 18.66 0.370 54 — 1.100 74.08 3.300 88 ^ 7 10.000 95.18 30.000 96.19 19.300 215 0.123 13.49 (Please read the precautions on the back before filling this page)-Binding-Binding.-妗， -456- This paper size is applicable to China National Standard (CNS) A4 specification (210X297); f) V. Description of invention (455) A6 B6 printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. FITC analysis of HIV-1 Amount of HIV-1 Protease Inhibition% HIV-i FITC KI (nM) 0.370 43.33 U00 76.11 3.300 97.93 10.000 107.1 30.000 98.49 27.800 216 0.123 &lt; 10 0.370 &lt; 10 L100 &lt; 10 3J00 &lt; 10 10.000 10.88 30.000 31.42 217 0.123 &lt; 10 0.370 &lt; 10 丨 .100 &lt; 10 3.300 31.61 10.000 64.15 30.00 72.93 218 0.123 &lt; 10 0.370 &lt; 10 1.100 26.24 3.300 65.18 10.000 88.04 30.000 91.38 219 0.123 52.1 0.370 80.99 1.100 92.55 3.300 100.02 10.000 108.63 30.000 97.33 10.400 220 0.123 &lt; 10 (Please read the precautions on the back before filling this page). #.. Binding-Binding--457- This paper rule applies to China National Standard (CNS) A4 specification (210X297 mm) V. Description of the invention (456) A6 B6 Compound number printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Example number HIV protease FITC analysis HIV-1 agent (uM) HIV-1 protease inhibition% HIV- 丨 FTTC KI (nM) 0.370 &lt; 10 1.100. 25.21 3.300 63.61 10.000 93.97 30.000 100.6 221 0.123 79.73 0.370 I0I .4 uoo 116.32 3.300 116.79 10.000 119.02 30.000 123J5 3.500 222 0.123 80.39 0.370 94.06 1.100 10328 3.300 110.48 ....... 10.000 110.71 _ 1 30.000 110.26 3.100 I 223 0.123 11.13 0.370 31.33 1.100 62.31 — 3.300 85.69 10.000 102.35 30.000 I0L49 71.600 | 224 0.123 &lt; 10 —.1 0.370 10.86 1.100 42.42 3.300 72.31 10.000 83.71 30.000 95.31 225 0.123 &lt; 10 -458- This paper size applies to China National Standard (CNS) A4 specifications (210x297 mm) ............................. ......................................................................... ..... Order. (Please read the notes on the back before filling in this page) A6 B6 V. Description of the invention (457) Compound number printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs Example number HIV protease FITC analysis 1 dose of u (uM) HIV-1 protease inhibitor% HIV-1 FITC K1 (αM) 0.370 &lt; 10 1.100 14.88 3.300 47.01 10.000 77.22 30.000 91.73 226 0.123 14.15 0.370 43.71 1.100 74.1 1300 87.57 1 0.000 100.72 30.000 103.62 18.900 227 0.123 &lt; 10 0.370 41.74 1.100 81.14 3.3uO 91.12 10.000 90.07 30.000 80.94 21.900 165 0.410 61.74 1.230 86.71 3.700 98.41 11.000 106.2 33.000 111.31 100.000 114.27 86 166 0.410 &lt; 10 U30 13.21 3.700 33. 100.000 100.02 167 0.410 83.16 .1 —459— {谙 Read the precautions on the back before filling in this page), install, you can. This paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) V. Invention Note (458) A6 B6 Compounds printed by employees of the Central Standards Bureau, Ministry of Economic Affairs, Consumer Cooperatives, Case No. HIV Protease FITC Analysis, HIV-1 Agent, (uM) HIV-1 Protease Inhibition% HIV-1 FITC ΚΙ (nM) 1.230 99.48 3.700 113.13 11.000 114.1 33.000 113.9 100.000 116.19 28 168 0.123 &lt; 10 0.370 12.38 1.100 46.35 3.300 74.89 10.000 94.67 30.000 107.35 135 169 0.123 &lt; 10 0.370 &lt; 10 1.100 13.07 3.300 44.38 10.000 76.82 30.000 99.88 164 0.123 &lt; 10 0.370 14.64 | 1.100 46.22 3.300 87.3 10.000 99.68 30.000 102.14 78 212 0.123 &lt; 10 0.370 &lt; 10 1.100 &lt; 10 3.300 32.53 10.000 59.51 30.000 69.5 367 0.123 &lt; 10 (谙 Read the notes on the back before filling in this page) . Binding.-:-,-

I * 3 V. Description of the invention (459) A6 B6 Compounds printed by employees of the Central Standards Bureau, Ministry of Economic Affairs, Consumers' Cooperative Compound S, case number, HIV protein, FITC analysis, HIV-1 agent, HIV-1 protease inhibition%, HIV-1 F1TC KI (ηΜ) 0.370 &lt; 10 1.100 23.67 3.300 58.55 10.000 86.14-30.000 101.6 366 0.123 &lt; 10 0.370 &lt; 10 1.100 40.33 3.300 72.93 10.000 92.17 30.000 106.62 368 0.123 &lt; 10 0.370 &lt; 10 1.100 17.39 3.300 54.46 10.000 77.77 30.000 86.75 370 0.123 &lt; 10 0.370 &lt; 10 U00 &lt; 10 3.300 &lt; 10 10.000 19.4 30.000 33.08 369 0.123 54.86 0.370 83.46 uoo 96.02 3.300 97.1 10.000 110.73 30.000 93.94 28 * 5 372 Q.123 65.28 —461 · * y ZX υ i 2 (Please read the precautions on the back before filling this page). Binding and binding. &Quot;, V. Description of invention (460) A6 B6 Compound number printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Example number of HIV protein and FITC analysis of HIV -1 Amount (uM) HIV-1 protease inhibitor% HIV] FITC ΚΙ (nM) 0.370 ^ 91.27 1. 100 104.8 3.300 108.35 10.000 108.6 30.000 106.29 5.87 373 0.123 31.82 0.37Q 68.9 LI00 86.98 3.300 97.07 10.000 102.4 30.000 104.95 18.3 371 0.123 86.78 0.370 108.97 L100 109.96 3.300 112.93 10.000 108.07 30.000 109.68 7,350 II 375 0.1_ 0.31 0.36 &lt; 10 3.300 57.38 10.000 78.95 30.000 86 377 0.123 &lt; 10 0.370 11.83 1.100 39.6 3.300 66.07 10.000 83.74 30.000 94.66 313 0.123 104.34 462 «This paper size applies to China National Standard (CNS) A4 specification (210x297 mm) ... ........................................ ....... Φ, ...... Installation (Please read the precautions on the back before filling this page)

A6 B6 V. Description of the invention (461) Example number of compound printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs ΗII protein FITC analysis HIV-1 agent fi (uM) HIV-1 protease inhibition 涔 HIV-1 FITC ΚΙ (nM) 0.370 96.49 LI00 100.61 3.300 100.19 10.000 105 «53 30.000 101.95 I.I70 356 0.123 97.71 0.370 97.24 1.100 97.9 3.300 10I.I7 10.000 102.05 30.000 100.33 1.320 38 1.000 18.65 10.000 83,17 100.000 93.37 113 1.000 39 ^ 8 10.000 99.82 100.000 10929 136 0.410 56.64 1.230 80.14 3.700 90.06 1L000 92.44 33.000 91.63 100.000 102.73 108 228 34.8 229 0.123 16.89 0.370 54.29 1.100 88.78 3.300 102.85 10.000 107.75 .463- (Please read the precautions on the back first and then fill in the clothes sheet) 0.-Binding. Binding.-Perch This paper size applies to China National Standard (CNS) A4 specifications (210X297 mm) V. Description of invention (Seven 2) A6 B6 Compound number printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economics Example number HIV protease FITC analysis | HIV-1 dosage &lt; uM &gt; HIV-1 protein Plum inhibition% fflV-1 FITC 1 KI (ηΜ) 1 30.000 Γ04.86 10.6 11.9 232 0.123 19.32 0.370 51.17 1.100 80.39 3.300 95.34 10.000 103.64 30.000 94.99 30.0 235 0.123 24.77 0.370 71.82 1.100 92.71 3.300 104J8 10.000 103.08 30.000 990.0 10.0 236 8.0 1 237 ... 丨 · 60.0 117.0 233 147.0 ..., / · 180.0 302.0 234 12.8 13.0 18.8 230 264.0 280.0 231 109,0 126.0 242 0.123 &lt; 10 -464 »· This paper size applies to Chinese national standards (CNS) A4 specifications (210x297 mm) {Please read the precautions on the back before filling in this page)-Binding and binding. A6 B6 Printed by the Consumer Standards Department of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the Invention (463) Compound S case number HIV protein PITC analysis HIV-imfi (UM) HIV-1 protease inhibition% Hiv-i rare KI (aM) 0.370 &lt; 10 UOO 13.81 3.300 35.96 10.000 65.35 30.000 78.92 386 0.123 &lt; 10 0.370 &lt; 10 1.100 14.33 3.300 35.35 10.000 64.45 30.000 96.28 243 0.123 &lt; 10 0.370 &lt; 10 1.100 &lt; 10 3.300 24.42 10.000 44.72 30.000 54.28 238 0.123 30.5 0.370 76.39 1.100 96.26 3.300 99.93 10.000 115.66 30.000 115.42 13.4 239 0.123 69.55 0.370 88.01 1.100 98.34 3.300 102.72 10.000 107.4 30.000 100.72 2.2 387-0.1465 t-lt; Please read the precautions on the back before filling out this page)-Binding and binding.-&Gt; ·. ^

I «· ^ A6 B6 V. Description of the invention (464) Compound No. printed by Shellfish Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. Example number of the protease FITC analysis HIV-1 agent egg (νιΜ) HIV-1 protease inhibition% HIV-1 FITC ΚΙ (nM) 0.370 &lt; 10 1.100 36.69 3.300 64.32 10.000 92.75 30.000 106.21 379 0.123 &lt; 10 0.370 48.64 1.100 84.49 3.300 96.22 10.000 106.83 30.000 113.1 18.3 240 0.123 54.87 0.370 89.42 1.100 111.38 3.300 113.39 10.000 114.19 5.0 34.2 241 0.123 81.78 0.370 91.77 1.100 98.65 3.3〇α 101.51 10.000 110.04 1.32 30.000 104.34 1.90 386 0.123 &lt; 10 0.370 &lt; 10 1.100 &lt; 10 3.300 19.2 • 10.000 45.45 30: 000 78.15 388 0.123 &lt; 10 9 —466— {Please Please read the notes on the back before filling this page.) Binding. This paper size applies to China National Standard (CNS) A4 specification (210x297). A6 B6 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs.

V. Description of the invention (465) Compound example number 1 &lt; ^ Protease? 11 (: Analyze HIV-1 molar mass (uM) HIV-1 protein plum inhibition% HIV-1 FTTC Kl (nM) 0.370 42.8 U00 76.04 3.300 96.45 10.000 98.23 30.000 93.72 21.7 389 0.123 &lt; 10 0.370 21.15 1.100 58.02 3.300 78.74 10.000 96.38 30.000 98.74 46.2 380 0.123 &lt; 10 0.370 21.48 U00 57.18 3.300 82,52 ιαοοο 103.26 30.000 107.7 87.9 384 0.123 12.21 0.370 47.4 1.100 79.24 3.300 92.88 10.000 102.72 30.000 101.92 24.1 381 0.123 &lt; 10 0.370 24 3.08 1.100 62 * 99.85 30.000 96.7 391 385 0.123 &lt; 10 I -467- (Please read the precautions on the back before writing this page}-binding, binding. This paper size applies to Chinese national standard. (CNS) A4 size (210x297mm ¢) ) B6 V. Description of the invention (466) Compound printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, Example No. HIV Protease FITC Analysis HIV-1 Agent 1 (uM) HIV-1 Protease Inhibition% HIV-1 FITC KI (nM ) 0.370 48.52 I.iOO 89.46 3.300 103.6 10.000 107.38 30.000 106 · 71 12.4 398 0.123 10 .47 0.370 40.87 UOO 74.23 3.300 91.47 10.000 105 * 24 30.000 105.17 4L5 397 0.123 35.71 0.370 92.92 L100 〖05.15 3.300 108.84 10.000 116.15 30.000 112.72 7.3 393 0.123 &lt; 10 ___j 0.370 &lt; 10 1.100 &lt; 10 3.300 37 * 51 10.000 30.000 89.76 392 0.123 &lt; 10 0.370 &lt; 10 1.100 11.47 3.300 47.01 10.000 77.59 30.000 99.66 282 0.123 &lt; 10 1 46 8— (Please read the precautions on the back before writing this page) This paper size applies the Chinese national standard ( CNS) A4 specifications (210X297 public directors) A6 B6 V. Description of the invention (467) Examples of compounds printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs HIV protein sea PITC analysis HIV-1 agent fi &lt; uM) HIV-l Protein Sea Inhibition% HIV-l FTTC KI (nM) 0.370 &lt; 10 UOO 10.56 3.300 43.22 10,000 65.32 30.000 96.32 315 0.123 80.69 0370 94.73 1.100 91.93 3,300 95.17 10,000 86.65 30,000 8139 2J8 J 365B 10.000 83.85 30,000 78.81 33.50 100 0123 94.03 3.30 0 87.33 10.000 92.56 30.000 89.11 365B 0.123 29.06 — 0370 56.47 1100 93.46 3.300 90.63 10,000 90.94 _ 30.000 85.31 14.3 353 0.123 61.39 0.370 92.71 UOO 102.79 -¾.- 3.300 110.06 10.000 113.06 -469- (Please read the precautions on the back first (Write this page) Binding. The ruled paper is changed to apply the Chinese National Standard (CNS) A4 specification (210X297mm) A6 B6 V. Description of the invention (468) Example of compound printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Protease FITC analysis HIV-1 (uM) HIV-1 protein sea inhibition% rav-ι fitc KI (nM) mooo 10λ2 2.4 350 0.123 22.25 0.370 64.26 1.100 82.19 1300 98.33 10.000 102.02 30.000 101.46 6.6 351 0.123 11.21 0.370 49.28 * UOO 76.6 3.300 93.86 10.000 97.8 30.000 95.76 16.4 354 0.123 71.38 0.370 86.43 1.100 96.07 ............ 3.300 100.46 10.000 103.33 30.000 108.2 1.45 383 0.123 &lt; 10 0.370 &lt; 10 ποο 28.86 3.300 72.98 10.000 90.2 30.000 94.63 390 0.12 3 &lt; 10 0.370 &lt; 10 1.100 13.14 3.300 43.57 10.000 66.38 1 tPlease read the notes on the back before filling in this page) Binding. The size of this paper is applicable to China National Standard (CNS) A4 specifications (210x297 mm) — 470— V. Description of the invention (469) Compound example number HIV protease PITC analysis HIV-1 dose (uM) ΗΠ-1 protein sea inhibition% fflV-1 FITC KI (nM) 30.000 85.2 391 0.123 &lt; 10 0.370 &lt; 10 1.100. &Lt; 10 3.300 28.32 10.000 59,13 30.000 84,2 400 0.123 17.41 0.370 54.76 L100 78.68 3.300 94.69 10.000 114J27 30.000 109.34 35.8 394 0.123 72.74 0.370 102 U00 109.48 3.300 115.21 10.000 119.6 30.000 122.96 6.04 399 0.123 &lt; 10 0.370 1-100 54.12 186 1 378 0.123 102.78 ........ 0.370 110.63 UOO 111.64 3.300 117.82 10.000 112.42 30.000 112,1 1,06 357 0.123 103.88 0.370 97.18 -471- A6 B6 Staff of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the cooperative V. Description of the invention (470) Compound example number HIV protein sea FITC analysis HIV-1 agent most (uM) HIV-1 protein sea inhibition% HIV-1 FTTC KI (nM) 1.100 101.03 3.300 98.28 10.000 96.83 30.000 89.6 0.62 355 0.123 117.42 0.370 117.25 1.100 115.36 3300 103.4 10,000 72.63 30.000 61.88 2.14 355 0,123 112.03 0.370 I10J8 1.100 107.13 3.300 109 ^ 6 10.000 110.07 30 · 000 108.3 1.06 374 0-123 121.27 0370 121.33 UOO 131.15 3.300 I24J6 v 10.000 12921 30.000 127 * 57 1.3 402 0.123 103.69 0,370 106.4 1.100 110.07 3.300 10022 10.000 98.03 30.000 98.47 0 0.123 46.49 0.370 88J8 (谙 Please read the precautions on the back before filling in this page}. See.-Binding. · Sheets of Paper Series 472- "Degrees a time material (GNS) Jiashige (21GX297 issued)" A6 B6 V. Description of the invention (471). Compound example number HIV protein sea FITC analysis | HIV-1 dose (uM) HIV-1 protease inhibition% HIV-1 FITC Kl (nM) 1.100 101.46 3.300 105.91 10.000 101.32 30.000 77.2 3.13 ........................................ ............... ... load ::: ...... Order ..! :! Yan, 1 (Please read the notes on the back before filling out this page} Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs -473- This paper size applies to China National Standard (CNS) A4 (210X297 mm)

Claims (2)

Patent No. 83100644 Chinese Patent Application Amendment (Yuan 87) A8 B8 C8 D8 A compound of formula ΐI supplement Its composition is 5 ^. R a R and a) Or practice 丨 | (Please read the notes on the back before filling out this page) RO 4 (c D ^ o, 1T Printing by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. Medium. d This paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) No. 83100644 patent application Chinese amendments to the scope of patent application (Jan 87) A8 B8 C8 D8 A compound of formula ΐI supplement Its composition is 5 ^. R a R and a) Or practice 丨 | (Please read the notes on the back before filling out this page) RO 4 (c D ^ o, 1T Printing by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. Middle. Ab Its other, c is 〇 1 d This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 VI. Application for Patent Scope Printed by the Consumers' Cooperatives of the Central Standards Bureau of the Ministry of Economics which is a) -H, b) -〇C η H 2 n * τ * c) -cf3, d) -〇-CnH2 „-ch = ch2, or e) -0-C η H 2 n -H et; or Rs to synthesize phenyl; or where R 〇 And R 2 to synthesize phenyl; wherein R 3 is a) CvH ^-CH — CyH》 1 \ R- IV b). -Di cage ethyl-, c) r-di cage vinyl-, d) -C Η -(C. ^-C &lt; 5-cycloalkyl) 2, e) -5,6,7,8,9-tetraaza-5H-S # cycloheptenyl f) -1.2,3.4 -tetrahydro-naphthalene -OCnHan-l, §) -CH f C. Η 2n + 1) -C (0) -〇-CnH2n + l, h) -C Η (C H 2-cage group) 2, i) -C ν Η 2 ν-C Η (R 4)-C ν Η 2 ν-het, or .j) -CvHav-CH (R4.)-CvH2V-het-R5; where R 4 is (please read first Read the notes on the back side and fill in this page), 1T This paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) D8 Patent application scope a) b) ~ CH2-C (0) -〇-CnH2n * lfc ) -c3-cscycloalkyl, or d) -C „H2„ -C3-Cecycloalkyl; where R 5. is a) -Η · b), c) -C (0)-C „H2… D) (ortho) or (meta)-0-C „Η 2 n-C Η = C Η 2 e) -Cx-Cs alkoxy, substituted by 0 or 1 hydroxyl group on each carbon atom , F) -0-C f 0)-C η Η 2 η ^ 1 »g) -B r &gt; h) -CN, ί) j) -Xl-CriHzn -halogen, k) _Xl_CnHan-NH2, I) -Xl.-CnH2n-NH-C ί0) -0-CnHzn-l m) -Xt-C „H? In-CH (NH-C (0) -0-CnH2n * 1) C (ΰ)-0- UH2 n X 'n) -Xi-CmH2 ™ -CH (NH-C (0) -0-Cr, H2n.a) -C η Η 2 η-Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please 闰Read the notes on the back and fill in this page) Η et, &gt; ο)-X 1-C „Η 2 η-C Η (N Η a) C 0 Π Η &gt; Ρ) -Xi-C.H2n-C (0) -0-CnH2r, this paper size applies Chinese National Standard (CNS) A4 (210X297 mm) 6. Scope of patent application. A8 B8 C8 D8 printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. ) -Xl-CmH2m-〇-aryl * t) ™ Xl-CmH2m-〇-CnH2n + a? U)-C m H 2 τη-X 1-C m H 2 m-H et, v) _Xi-CnH2n &quot; C (0) -Het J w)-X \-C n H 3 n-C (0)-NH-C n H 2 n-H et &gt; x) -Xi-CnH ^ nS-Het jy)- CmH2ni-Xl-〇-Cn H2n-aryl * Z) -CTnH ^ m-Xl-〇-CnH2n- H et »a 1) -X x-H * bl) -Xi-CH = CHa &gt; cl)- X i-CH = CH -aryl * dl) -Xi. ~ N (Rd〇) 2 &gt; el) -X 1-C η H 2 „-phthalocyanine tf 1) -Xt .- (pentabenzene Group, g 1) -X 1-C η H .2 ”-bicyclo [2.2 • 1] heptane hi) ~ CM-H 2, J-R 3 〇, i 1) -N = C-(NH- CH (C n H… T) 2) 2 5 J1) -NH-P (0) (Ry) -aryl, kl) -NH-P (0) (0-R, t) -aryl, m- NH-C (S) -NH-RA2, or ml) -NH-C fS) -CH2-R ^, &gt;; where) U is -4-This paper size applies Chinese National Standard (CNS) A4 specifications ( 210X297 mm) (Please read the notes on the back before filling this page) A8 B8 C8 D8 VI. Application scope -a) -Η H-C (0)-&gt; b) -C (0)-NH-, c) -NH ~ S〇2-1 d) -s〇2 -nh- »e) -nh-s〇2-hh- &gt; f) -c (0) -0-, g) -〇 ~ C (0)-* h) -N (C n H 2„- Aryl) -C (0)-, n -HH-C (0) -HH- &gt; or j) vertical] _ S 0 2 (Please read the notes on the back before filling out this page) .11 of which Is from 0 to 5; where η is from 1 to 5; where P is from 1 to 8; where q is from 0 to 5; where r is from 1 to 8; where s is from 1 to 6; where t is from 1 to 1 2; where u is from 2 to 6; where v is from 0 to 2; where aryl is a) cage is 0 to 3 R b substituted, b) naphthyl is 0 to 3 R β substitution, or c) _ cage is 0 to 3 R β substitutions; where He f. Is a 5-or 6-membered saturated or unsaturated ring, containing from 1 to 3-5-This paper size applies to China Standard (CNS) A4 specification (210X297 mm) 17. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 6. Patent application scope: False heteroatoms selected from the following including nitrogen, oxygen and sulfur; and including any bicyclic group, Any of the above Fused to a stupid ring or another heterocyclic ring; and the ring may be connected via a carbon on the ring or a second nitrogen or an out-of-ring nitrogen; and if chemically appropriate, the nitrogen atom may be protected; and 0 to 3 substituted by R 7; 1 and R 7 may be independent a) -C t -C 5 alkyl, substituted by 0 to 3 halogens, or substituted by 0 or 1 hydroxyl group on each carbon atom, bV -OH &gt; c) _ C '_ C 5 fluorenyl_ 0 fi, d) -O-Ct-Cs alkyl, substituted by 0 to 3 halogens, or 0 or 1 hydroxyl group on each carbon atom Replace, (Please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs e) -O-Ca-C ·? Huiji is 0 or 1 f) Halogen, g) -NH2, h) -N Η-C 1.-C! 5 Hexyl, η mono- or di-C i-C s alkylamino-NH-OH &gt; k) -N (CH 2-0 H) 2, I ) -C (0) -NΗZ &gt; m) -C (0) -C: i-C5 焼 group, n) -CH0 &gt; o) -COOH &gt; P) -cnx2, this paper uses China country Standards (CNS> A4 specifications (210X297 mm) A8 B8 C8 D8 Patent application scope Central employees of the Ministry of Economic Affairs Central Bureau of Consumer Consumption Cooperation Indication q) Nitro, r,) -CN, s) -S03H, t) -S02NH2 &gt; u) -S02-phenyl is 0 to 3 V) groups substituted by R 1 2 and is 0 to 3 R 1 2 w) -SiU-HH- cage base is 0 to 3 R ζ 2 X) -0 [(CH3) 20] .CH3 &gt; y) -C f 0)-0-C n Η 2 η + 1 yz) -N HC (0)-C η Η 2 η + 1 'a Π -C „H an-NH-C (0) -fluorenyl, bl) -N = N- S group is 0 Or 1 -M cl) isoxazolyl * dl) pyridyl, el) -Xs-CuH- ^ u- R 3 Ο * f 1) morpholinyl; gl) hexahydropyridyl i hi) hexahydro Yang: Gengji) i 1) -NRaoRa ^ 'jl) -0 R 4. 〇' kl) --- NH- \ &gt; S〇2 X or (CH2) u 1-11) -C η Η ^ η- 〇- C η Η Π-〇C π Η 2 η 1 »Superseded by --------- ΦI— (Please read the precautions on the back before filling this page) The size of the paper used in this edition applies Chinese national standards ( CNS) A4 specification (2! 0X297 mm) 6. Scope of patent application A8 B8 C8 D8 printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs where) U is -NRa. ! ^ Where) (3 is a) -0- * b) &quot; CH 2-0-* c) _S〇2NR40_ * d) &quot; NR40SO2- * e) -C (0)-, f) • C ( 0) NR 4 0-, g) -u⑻, or h) -NR 4 〇-; where R θ is a) -Η,: 〇)-C „Η 2 -phenyl, which is 0 to 3 R β Substitution, C)-C η H a η-H et &gt; d)-C n Η 2 „-C 3-C β cycloalkyl, e) — 1, f)-C n-H„ n-CH = CH 2 ^ g &gt;-LH 2 s + 1 is substituted by 1 or 2 hydroxyl groups, h)-C Η 2-epoxide, Ο -c „h2„ -oxiranyl group,-(CnH2n-0 ) n-CnH2n + l 5 k)-C (Ο)-C s H 2 s + 1, or 1)-C Η (Ο Η)-C 3-C · 5 cycloalkyl; where 1 is the paper size Applicable to China National Standard (CNS) Α4 specification (210X297 mm) (Please read the precautions on the back before filling this page) A8 B8 C8 D8 VI. Application for Patent Scope Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, a) -C-C 4 alkyl, b) aryl; where Ru is, a) -Η * b) -Ci_C4 complex, c) aryl, or d) which is pharmaceutically acceptable where R "is a) 1.-C 3 Izo, b) C 1.-C 3 Ioxo c) Dimethyl Junki, d) Diethyl saddle Base, e) CF 3 &gt; f) CN »g) S, h) -NHa &gt; i) -OH, j) -C⑻-, or k) -S0v &gt;-HHa-; where 1? 3 Ο is a ) Malford Command Volume, b) Hexapyridyl, c) Hexaprazine, d) (Please read the notes on the back before writing this page) The size of this paper is applicable to Chinese National Standard (CNS) A4 (210X297 mm) 6. Scope of patent application Λ β) -OR 4.0 5 f) —NH-X. \ / (CH2) ug) -K-methyl-hexa Hydropyridyl, or h) halogen; 1U. And Re is' independent a.)-Η or b) -C Τ-C 4 alkyl; R 4 2 is a) C 1 -C 4 alkyl, or b) a cage group; the restriction is: 1) When R 1. And R ;? 〇 to synthesize Formula II, and each of RR 2 is -Η &gt;-F or -〇- c „Η 2 η ♦ 1. and R 3 is the moiety of Formula ί V and R 4_ -C Η 2 + · !. or cyclohexyl, then RS is not -Η, .halogen or -〇C η Η 2 η-1; 2) When Ri? Is-m_Xl_〇-CnH2n_ aryl, the central standard of the Ministry of Economic Affairs Printed by the Bureau's Consumer Cooperative (please read the precautions on the back before filling this page) -C nm-X '-11-c „Η 2„-Het or X i-N (R 4.) 2, X 1 Non-CfO) -NH- »-HHSOa- &gt; -S02-HH-« -NH-SOz-KH- · -C (0) -0-, -NH-C (0) -NH- or-Ν ( (: „Η2γι-aryl) -S02-; 3) When R 4 is -H in the part of formula IV, R 5 contains a substituent of X i, where Xτ is-MKS02-; 4) when -X t-C „P, 2-Ο -aryl or uu ·„-X— τ:-c ™ Η 2 m-Ο -1% Η 2 η + T. If Iti is 〇, then X t is not ι ο- Paper size adopts Chinese national standard (CNS> A4 specification (210X297 mm) A8 B8 C8 D8 VI. Patent application scope -C (0)-Η Η-.-Η HS Ο 2-*-S Ο 2-Η Η -&gt;-Ν Η-S Ο 2-Η Η-* -C (0) -0-, -NH-C (0) -NH-, -N (CnH ·: ^-aryl) -S02- or -N (C m Η? M-C rv Η 2 rv * Τ.-S 0; 5) R 3 is a dibasic ethyl group or a distyryl group, but when R ^ 〇 and R 2 〇 are synthesized UI parts; 6) when 10 and R 2 are synthesized by formula II Part, and 1 ^ and (^ are independently -Η &gt;-F 5¾-0 C. Η 2 „. X ^-Η Η 2 * Beii R 3 non-CHH +!)-C ⑻-il-C „Η… τ; and 7) when Ri. And Rs〇 to form a part of Formula I, and R. , Ri and R__j are each -Η, then 1 to 3 is neither 5-("-3 alkoxy) -1,2, 3,4 -tetrahydro-1 -naphthylene 'nor is it a part of formula IV , Where V is 0, R s is -Η, halogen or methoxy} group, and R 4 is polyester-C Η 2-C 0 0 (C i-3 alkyl); when R w and synthetic formula ΐ I part And R0, 1 and R2 are each fluorene, but not 3-methylene-4-hydroxybenzopyran-2-one; and a pharmaceutically acceptable class thereof. 2. Hamamatsu applied for a patent The compound of the range item 1, in which R ^ 0 and the synthetic formula UT part. 3. The compound of the formula I according to the scope of the patent application_item 1, in which R is flying. And the synthesis of R -ρ_ η --- ---- (Please read the notes on the back before filling out this page) Order printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs -11-This paper size applies Chinese National Standard (CNS) A4 specification (210X: 297 mm) A8 B8 C8 D8 The scope of patent application where R 1 is a)-Η, or b)-0 C η Η 2 n ». Where R 2 is a) '-Η »or b)-0 C„ H an where R 3 is V, SK (please read the notes on the back before filling this page). Packing: # ， ΤΓ b) -5, 6, 7,8,9 -tetrahydro-5 H-benzocycloheptenyl where 1U is a) -cyclopropyl, or b) + l I line where R s is 3) -Η * b) -XI-C η Η C) -X- C n Η d) -X 1-C η Η e) KH f) -X 1-C π. Η In Xl is -NH-C 12 This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 feet) 6. The scope of patent application where m is from 2 to 4; where η is from 1 to 4. 4. The compound according to item 1 of the scope of patent application, which is selected from the group consisting of 3- (1- (4-bromophenyl) -2-methylpropyl) -4-hydroxycoumarin , Butyric acid, 2- (4-hydroxy-2-oxy-2H-1-benzopiperan-3 -yl)-, ethyl I, 3-U, 2-diphenylethyl) -4- Hydroxycoumarin, 4-hydroxy-3- (2,2-diphenylethyl) -coumarin, 3- (cyclopropylphenylmethyl) -4-hydroxycoumarin, 3- (2 -Cyclohexyl-1-phenylethyl) -4 -hydroxycoumarin, coumarin, 4-hydroxy-3- [1- (4-propanylphenyl) propyl]-, 3-U, 2-diphenylvinyl) -4-hydroxycoumarin, coumarin, 7-trifluoromethyl-4-hydroxy-3- (1-phenylpropyl)-, coumarin, -fluoro- 4-hydroxy-3- (1-fluorenylpropyl) .-,, coumarin, 3-[1-(4-bromophenyl) propyl] -4 -hydroxy- * coumarin, β-fluorene 4-Hydroxy-3-(1-benzylpropyl)-, coumarin, 4-hydroxy-3- [1- (4- (2,3-dihydroxy) propoxyphenyl] propyl Base]-, printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs (please read the precautions on the back before filling this page) Coumarin, 3 -[1-(3-Alkylcyl) propyl] -4 -hydroxy-, 2N-naphtho [l, 2-b] piperan-2-copper, 4-hydroxy-3- (branthylpropyl )-, Coumarin, 3- [1- (3-cyanophenyl) ethyl] -4 -hydroxy-, coumarin, 3- [1- (3-aminophenyl) propyl] -4 -Hydroxy-,-13-Hydrochloric Acid-This paper size applies to the Chinese National Standard (CNS) A4 (210X297 mm) A8 B8 C8 D8 Six, patent application scope salt, * 4-hydroxy-3- [cx- Third butoxycarbonylmethyl] benzylcoumarin, 3- (1 (3-allyloxyphenyl) propyl) -4-hydroxycoumarin, 3-(1 '-(3-bromobenzene Propyl) -4-hydroxycoumarin, 3- (1 '-(3--((2, 3-dihydroxy) propoxy) phenyl) propyl) -4-hydroxycoumarin, U , -U-ethetyloxybenzyl) -propyl) -4-hydroxyacoumarin. 3-Cyclopropylcylmethyl-4-hydroxy-7-methoxycoumarin, 3- Π '-(2-ethethoxyfluorenyl) propyl) -4-hydroxycoumarin, 3-U'-(2-allyloxyphenyl) propyl) -4-hydroxycoumarin, 4-hydroxy-3- (5-6,7,8,9-tetrahydro-5H-benzocycloheptenyl) -coumarin, coumarin, 3-[ 1-[3-[[[(2-Benzoxazolyl) methyl] amino] carbonyl] cyl] ethyl] -4-hydroxy-, coumarin, 4-hydroxy-3-[l- [3-[[[(2-pyridyl) methyl] amino] carbonyl] phenyl] ethyl]-, coumarin, 4-hydroxy-3-[1-[3-[[(phenylmethyl Base) amine] carbonyl] cage 巻] 碁--, printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) 'Benzyl Saddle, N- (2,3- Dihydro-2-hydroxy-1 «-hydrofluoren-1-yl) -3- [1-f 4 -hydroxy-2 -oxy-2 fluoren-1 -benzo. Mannan-3 -yl) ethyl]-, 芊 _ 睽, 3- [1- (4-hydroxy-2-oxy-2 2-1--1-clotanan-3-yl) ethyl] -N- [2 -Methyl-1-[[(2-pyridylmethyl) anthryl] carbonyl] butyl]-, 4-hydroxy-3-[1-[3-[[[(1, 1 -dimethylethyl Oxycarbonyl) methyl] amine-14-This paper size applies to the Chinese National Standard (CNS) A4 specification (210 &gt; &lt; 297 mm) A8 B8 C8 D8 VI. Patent application scope base] carbonyl] phenyl] ethyl] -Coumarin, t-coumarin, 3- [1- [3-[(butylamino) carbonyl] phenyl] ethyl-4-hydroxy— &gt; coumarin, 4-meryl-3- 3- [ l- [3-[[[[((4-Mamorpholinyl) carbonyl] methyl] amino] carbonyl] phenyl] ethyl]-, 'coumarin, 3-Π- [3-[[[ [[[(2-Benzosulfalyl) methyl] amino] carbonyl] methyl] amino] carbonyl] benzyl] ethyl] -4-hydroxy-, coumarin, 4-hydroxy-3- [l- [3-[[U -Naphthyloxymethyl) carbonyl] amino] phenyl] propyl]-, fluorenylcarboxylic acid, Π-[[[[[3- [1- (4-hydroxy-2- Oxy-2H-1-benzopiperidin-3-yl) propyl.] Phenyl] amino] carbonyl] -2-methylpropyl]-, ί, 1-dimethylethyl ester,, Coumarin, 4-hydroxy-3-3-Π- [3-[[[[(1 1-dimethylethoxycarbonyl) fluorenyl] methyl] carbonyl] fluorenyl: 1¾yl] propyl]-, 4-hydroxy-3-[1-[3-[(boxy-3 -cyl Propyl ') amino] cage] propyl] -coumarin, coumarin, 4-hydroxy-3- [1- [3- [U-fluorenyl) amino] phenyl] propane-L «. 'Coumarin, 4-hydroxy-3-[l- [3-[[(2-pyridyl) carbonyl] amino]] Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back first) Fill out this page again) $ yl] propyl]-, coumarin, 3-Π-[3-[[(aminomethyl) carbonyl] amino] phenyl] propyl1-4 -hydroxy-, tri Fluoroacetate, coumarin, 4-hydroxy-3-[1-[3-[[1 -oxy-3 -methyl-3- [Π, 1-dimethylethoxycarbonyl) amino] butyl Base] amino] phenyl] propane-15-This paper size applies to Chinese National Standards (CNS) A4 specifications (210X297 mm) A8 BS C8 D8 Six, patent application scope, • 4-hydroxy- 3- [l- [3-[[3-[(l, l-dimethylethoxycarbonyl) amino] -1-ketopropyl] -amino] benzyl] propyl] -coumarin, coumarin, 3 -[1- [3-[(3-Amino-3-methyl-butylammonium) amino] rongyl] propyl] -4 -hydroxyl -, Trifluoroacetate, 3- [1- [3-[(3-amino-1-ketopropyl) amino] phenyl] propyl] -4-hydroxy-coumarin, trifluoroacetate , Coumarin, 4-hydroxy-3-U- [3-[(l -oxy-3-phenylpentyl) amino] $ yl] propyl]-, coumarin, 4-hydroxy-3 -[1- [3-[[4-[(1,1-dimethylethoxycarbonyl) amino] -1-ketobutyl] amino] phenyl] propyl]-, 丨 &gt; Acid, N 2-[(1,]-dimethylethoxy) carbonyl] 1- [3- [1-(4-hydroxy-2 -oxy-2 fluorene)-:!-Benzopiperan-3 -Yl) propyl] phenyl]-, 1,1-dimethylethyl g, L-glutamic acid, N-[3-[1-(4-hydroxy-2 -oxy-2 Η- : 1-benzopiperan-3 -yl) propyl] benzyl]-, 'mono (trifluoroacetic acid) salt, chrysin, 4-hydroxy-3- 3-Π- [3-[(1-oxy -4-Phenylbutyl) amino] cage] propyl]-, printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back before filling in this education) Coumarin, 4-hydroxy-3 -[l- [3- [U-oxy-5 -phenylpentyl) amino] cagel] propyl]-, coumarin, 4-hydroxy-3- [b [3-[[(笨Methyl) hydroxy] amino] cagel] propyl 1-, Beans, 3-Π- [3-[(3-cyclohexyl-1-_propyl) amino] phenyl] propyl] -4-hydroxy-, -1ί5-This paper is sized to the Chinese National Standard (CNS ) A4 specification (210 × 297 mm) A8 B8 C8 D8 6. Application scope: Coumarin 5 4 -Hydroxy-7 -methoxy-3- [1- [3-[(Buxy-3-benzene Propyl) amino] phenyl] propyl]-, coumarin * 4-hydroxy-3-[l- [3-[[3-[(l, l-dimethylethoxyyl) Amine] -butanylpropyl] amino] phenyl] propyl] -7-methoxy-, 1-pyrimidincarboxylic acid, 2-[[[3-Π- (4-hydroxy-2- Oxy-2H-1-benzoxan-3-yl) propyl] phenyl] amino] carbonyl]-, 1, dimethyldimethylethyl, aminocarboxylic acid, [2-[[3- [ 1- (4-hydroxy-2-oxy-2P-1-benzopiperan-3-yl) propyl] phenyl] amino] -methyl-2-copperethyl]-, 1, dimethyldimethyl Ethyl ethyl ester, Protamine, 2-Amino-fluorene-[3-[1-(4-hydroxy-2 -oxy-2 fluorene-1 -benzopiperan-3 -yl) propyl] cage Group]-, mono (trifluoroacetic acid) salt, coumarin, 4-hydroxy-3- 3- [1- [3-[[3- (4-hydroxyphenyl) -1-onepropyl] fluorenyl 1 cage Propyl] propyl]-, coumarin, 4-hydroxy-3-Π- [3-[[3- (1 -Indol-1-yl) -1-amidinopropyl] anyl] cagel] propyl]-, coumarin, 4-hydroxy-3-[l- [3-[[3-U-naphthyl ) -Bu copper propyl] anthryl] poly]] propyl]-, 4-hydroxy-3-(1- (6-methoxy) -1,2, 3,4-tetrahydrozeiyl) -fragrant Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Bean Economics (#Firstly read the notes on the mouth and fill in this education), 4 -hydroxy-3-(1-(7 -methoxy) -1, 2, 3 , 4-tetrahydronaphthyl) -coumarin, coumarin, 3-[1-[3-[[3-[(2 -benzothiazolyl) tellurium]-1 -fluorenyl. 1 amino group ] Cage] propyl] -4-hydroxy-, -17-This paper size is applicable to China National Standard (CNS) A4 (210X297 mm) 6. Scope of patent application, 3- (dicyclopropyl) methyl 4-hydroxycoumarin, coumarin, 7- (allyloxy) -3- (ct-ethylbenzyl) -4-hydroxycoumarin, 3-[α -ethyl-[[[ 2-(indole-3 -yl) ethyl] carbonyl] amino] narrow] -4-hydroxy-, coumarin, 3- [bis (cyclopropyl) methyl] -4-hydroxy-7- Methoxy ... Coumarin, 3- (α-ethylbenzyl) -4 -hydroxy-7- (1-methylethoxy)-, coumarin, 7-ethyl -3- (cr-ethylbenzyl) -4-hydroxy-, vinylacetate (3- (1-(4-hydroxy-2 -oxy-2 fluorene-chromene-3 -yl) propyl ) Cage group)-amine; or [2-[[[[[[[[[3- [1- (4-Hydroxy-2 -oxy-2Η-1-S-piperazin-3-yl) .propyl] phenyl] Amine] sulfonyl] vinyl]-, ethanesulfonic acid, (3- (1- (4-hydroxy-2-oxy-2Η-chromen-3-yl) propyl) phenyl) -vinyl Amine; or [2-[[[3- [1- (4-hydroxy-2-oxy-2H-benzobenzopiperan-3-yl) propyl] benzyl] amino] sulfonyl] ethyl Group]-, 2-Π, 3 -bis_-1, 3 -dihydro-isoindole-2 -yl) -ethanesulfonic acid (3-(W4-hydroxy-2-oxy-2 fluorene -color Alkenyl-3-yl) propyl) -phenyl) fluorenamine; or [2-"[[3-[1-(4-hydroxy-2 -oxy-2 fluorene-1 -benzopiperan-3- Propyl] propyl] cagel] amino] sulfo_yl] ethyl] -phthalide_imine]-, and printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 2-(Ν -third butoxycarbonyl-amino) -ethanesulfonic acid (3.- (1--(4-Ethyl-2 -oxy-2'-chromene-3-yl) propyl)- (Benzyl) -hipamine; or urethane, [2-[[[3-U-(4- -2 - yloxy -2 Η - 1 - benzopyran -3-- yl) propyl] Cage-yl] amino] Qi Qi Niang] ethyl] -, 1, BU-dimethylethyl ester. 5- The compound based on item 3 of the scope of patent application is selected from the group consisting of the following sisters: 18 This paper is applicable to Chinese national standards (CNS> A4g (210X297 mm)) 6. Scope of patent application • 3- (ring Propylphenylmethyl) -4-hydroxycoumarin, coumarin * 4-hydroxy-3- [1- [3- [[[((1,1-Disylethoxycarbonyl) amino] amino Group] carbonyl] amino] phenyl] propyl]-, coumarin, 3-Π- [3-[[(aminomethyl) carbonyl] amino] phenyl] propyl] -4-hydroxy-, Trifluoroacetate, 4-hydroxy-3- (5-6,7, 8,9-tetrahydro-5Η-benzocycloheptenyl) -coumarin, coumarin, 4-hydroxy-3- 3- [ 1- [3-[[4-[(Ί, 1-dimethylethoxycarbonyl) anthryl] -1-ketobutyl] amino] phenyl] propyl]-, L-glutamic acid, N -[3- [l- (4-hydroxy-2-oxy-2-2--1-benzopiperan-3 -yl) propyl] phenyl]-, mono (trifluoroacetate), 3-cyclopropane Gytenylmethyl-4-hydroxy-7-methoxycoumarin, coumarin, 4-hydroxy-7-methoxy-3- 3- [1- [3-[(1-oxy-3- Phenylpropyl) amino] phenyl] propyl]-, coumarin, 4-hydroxy- 3- [l- [3-[[3-UH-indol-1-yl) -bupropionyl 1 saddle) benzene ] Propyl]-, Coumarin, 3-(α-ethylbenzyl) -4 -hydroxy-7- (1-methylethoxy)-, printed by the Consumer Cooperative of the Central Bureau of Standards, Ministry of Economic Affairs ( Please read the notes on the back and fill in this 莨) 4-Hydroxy-3- [1- [3-[[3-Π, 1-dimethylethoxycarbonyl) fluorenyl] -1-_propyl] jun Yl] cagel] propyl] -coumarin, coumarin, 4-hydroxy-3-[1- [3-[[3-[(1,1-dimethylethoxycarbonyl) aminopropylpropyl ] Amino] phenyl] propyl] -7-methoxy, aminosuccinic acid, [2-[[3-[1-(4-hydroxy-2 -oxy-2 hydrazone-1 -benzypiperazine嘀 -3 -even) Propionyl]] fluorenyl] fluorenyl] -1 -fluorenyl-2 -ketoethyl]-, -19-This paper size applies to China National Standard (CNS) A4 specification (210 × 297 mm) A8 B8 C8 D8 VI. Application scope of patent 1.1-Dimethyl ethyl ester, propylamine, 2-amino-H- [3_ [l- (4-hydroxy-2-oxybenzopiperan-3 -Yl) propyl] cryl]-, mono (trifluoroacetic acid) (salt), and coumarin, 7-ethoxy-3- (α-ethylbenzyl) -4-hydroxy-. 6. A peony drug product for inhibiting the retrovirus in mammalian cells infected with human immunodeficiency virus (HIV), comprising a pharmaceutically acceptable carrier and an effective dose selected from the group consisting of Compounds of the following composition group: 4-hydroxy-3- (α-methylbenzyl) -coumarin, 4-hydroxy-3 -phenylethylcoumarin, 4-hydroxy-3- (3-benzene Propyl) coumarin, 4-hydroxy-3-diphenylmethylcoumarin, 4-hydroxy-3-(3-hydroxy-1 -phenylbutyl) coumarin, 4-hydroxy-3 -(2-methyl-phenylphenylpropyl) coumarin, 4-hydroxy-3-Π-¾ylbutyl) coumarin, 4-hydroxy-3 -Π-cylbutyl) -coumarin * 4-hydroxy-3'-Phenylpentylcoumarin, 4-hydroxy-3-(: 3-methyl-p-benzylbutyl) coumarin, 4-hydroxy-3- (2- Benzopropyl) Coumarin, printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) • 4-hydroxy-3-Π, 3 -di cageylpropyl) fragrant Coumarin, 4-hydroxy-3-Π-U-methylbenzyl) -butyl) coumarin * Coumarin, 4-hydroxy-3- 3- [l -(4-hydroxyphenyl) propyl] 4-hydroxy-3- (1- (1-naphthyl) -propyl) -coumarin, coumarin, 4-hydroxy-7-methoxy-3 -U -Phenyl boundary group)-, -20-This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 public director) A8 B8 C8 D8 6. Scope of patent application • Coumarin, 4-hydroxy-6- Methoxy-3-U-phenylpropyl)-, myristotin, 4,7-dihydroxy-3- (1-benzylpropyl)-, coumarin, 4,6-dihydroxy-3 -(1-phenylpropyl)-, coumarin, 4-hydroxy-7-methyl-3- (1-phenylpropyl)-, coumarin, 7-chloro-4-hydroxy-3- U-phenylpropyl)-, coumarin, 4-hydroxy-3- 3- [l- (4-methoxyphenyl) propyl]-, coumarin, 4-hydroxy-3-Π- (3 -Hydroxyphenyl) propyl] u. • 4-hydroxy-3-U-phenyl-2-propenyl) -coumarin, coumarin, 3- (or-ethyl-para-fluorobenzyl ) -4 -hydroxy 4-hydroxy-3- [1- (1,2,3,4-tetrahydro) -naphthyl) -coumarin, 4-hydroxy-3- [1-hydropropyl coumarin , And 4-hydroxy-3 -U-phenylpropyl) -coumarin. 7 · The compound of formula I in item 1 of the patent application scope of the root beat, wherein R ,. And R 2 〇 synthesis (please read the precautions before filling in this page) R8 Printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs v, or 21-This paper size is applicable to China National Standards (CNS) A4 (210X297 mm) 6. Scope of patent application 'b) -CH- (cyclopropyl) 2 where I is 3) ~ CnHzn-il * 5¾ b) -cyclopropyl; where .R 5 is .-Η; where 1U is a} -H, b) -C n H 2 n-CH = CH2, c) -c… H… 1, d)- c „H2n-cyclopropyl, e) -CH (〇H) -c 2 η + Ί * or n -Cn Η"-tetrahydrofuranyl; (Please read the notes on the back before filling out this page) where η is from 1 to 5; where P is 従 3 to 5. 8 · The compound in the scope of patent application of Genbo is selected from the group consisting of: 6,7-dioxo-4 -hydroxy-3 -U- Phenylpropyl) -Cyclopent · [b] Piran-2 (5 Η)-嗣, printed by 3- (cyclopropylphenyl_.methyl) -6,7 printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs -Digas-4-meryl-cyclopenta [b] manan-2 (5 Η +)-嗣, 5,6,7,8-tetrahydro-4-hydroxy-3- (1-phenylpropyl) -28-1-benzopiperan-2-one, 3- (cyclopropylcylmethyl) -5,6,7,8-tetrahydro-4-hydroxy-211-1-benzopiperan- 2-嗣, -22-Application of this paper size National Standards (CNS> Α4Β (210X297 mm) 8 8 8 8 ABCD VI. Patent application scope '6.7, 8,9 -tetrahydro-4-hydroxy-3- (1-phenylpropyl) -cyclopenta [b ] Piper-2 (5H) -_, 3-(cyclopropylbenzylmethyl) -6,7,8,9 -tetrahydro-4-hydroxy-cycloheptan [b] piran-2 (5H) -Ketone, 5, 6, 7,8,9,10-hexahydro-4-hydroxy-3- (1-benzylpropyl) -2H-cyclooctane [b] nanan-2 -Ping 1, 3- ( Cyclopropyl cage methyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-2 H-cyclooctyl [b] piperan-2-hydrazone, 3- (dicyclopropyl (Methyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-211-cyclooctane ['b] anan-2-one, 3- (3-U-benzyloxyvinylamine ) -Phenyl) -cyclopropyl-methyl) -4 -hydroxy-5, (5,7,8,9,10 -hexahydro-cyclooctyl [b] piperan-2-_., 3- (Cyclopropyl-phenylmethyl) -4-hydroxy-6,7,8,9,10,11-hexahydro-5H-cyclooctane [b] mannan-2 -fluorene, 3- (cyclopropylbenzene Methyl) -5,6,7,8,9,10,11,12-octahydro-4-hydroxy-2 fluorene-cyclododecyl [b] piperan-2 -fluorene, 3- (cyclopropyl !! 5 s phenylmethyl) -5,6,7,8,9,10,11,12,13,14-decahydro-4 -hydroxy-2 fluorene -cyclododecane [b] piperan-2-嗣, printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) , 9,10-hexahydro-cyclooctyl [b] pyran-2-fluorene, 10-benzyl-3-dicyclopropylmethyl-4-hydroxy-5, β, 7,8,9,10 -Hexahydro-cyclooctyl [b] nesan-2-_, • 8-cyclopropylmethyl-4-hydroxy-3- (buphenylpropyl) -5,6,7,8-tetrakis-color Rare -2-Copper, -23-This paper size applies to Chinese national standards (CNS &gt; A4 size (210X297 mm) A8 B8 C8 D8 6. Application scope of patents. 9-Cyclopropylmethyl-3- (Cyclopropyl -Phenylmethyl) -4-hydroxy-6,7,8,9-tetraoxo-51 {-cyclo | ^; [^ &gt;] nan-2-one, N- (3- (cyclopropyl -(4-hydroxy-2-oxy-5,6,7,8,9,10-hexahydro-2H-cyclooctyl [b] piperan-3-yl) -methyl) -phenyl) -N ', N "-diisopropylfluorene, 3- (bubenzyl-2-phenylethyl) -4-hydroxy-5, 6,7,8, 9, 10-hexahydro-cyclooctyl [b] nanan- 2-keto, 4-hydroxy-10-methyl-3-U-phenylpropyl) -5,6,7, 8, 9,10 -Hexahydrocyclooctane [b] anan-2-one, 9-but-3-enenyl 3- (cyclopropyl-benzyl-methyl) -4 -hydroxy-β, 7, 8, 9- Tetrahydro-5 fluorene-cyclo.hepta [b] nean-2-fluorene, 10-cyclopropylmethyl-3- (cyclopropylphenylmethyl) -4-hydroxy-5, 6, 7,8, 9,1. 0-hexahydro-cyclooctyl [b] piperan-2 -fluorene, 3-(cyclopropylcylmethyl) -1 0-ethyl-4 -hydroxyl, -5, 6,7, 8, 9, hexaoxo-cyclooctyl [b] Xanan-2-fluorene, 3- (cyclopropyl-benzylmethyl) -4-hydroxy-yl-1 0-propyl, pyrene-5,6,7 , 8,9, 1 0 * · Hexahydro-cyclooctyl [b] Nanan-2 -fluorene, 10-butyl-3- (cyclopropyl-benzylmethyl) -4 -meryl-5,6, 7, 8,9, 10 -Hexahydro-cyclooctane [b] piran-2-嗣, printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 3- (cycling Propyl-phenylmethyl) -4-hydroxy-10-U-hydroxypropyl) -5, 6,7,8,9,10-hexahydro-cyclooctyl [1]] nan-2-_, 3 -(Cyclopropyl-benzylmethyl) -4-hydroxy-10-isobutyl-5, β, 7, 8, 9,10 -Hexachloro-cyclooctyl [b] nanan-2-copper, 3- (Cyclopropyl-rongylmethyl) -4 -hydroxy-1 0-(3-methylbutyl) -5, -2 4-Paper Standards are applicable to China National Standard (CNS) A4 specifications (210X297 mm). 6. Patent Application Park 6.7,8,9,10-hexa M-cyclooctane [b] piperan-2-copper, 3- (cyclopropyl -Phenylmethyl) -4-hydroxy-10- (tetrahydro-furan-3-ylmethyl) -5,6, 7, 8, 9, 10 -hexahydro-cyclooctyl [b] piperan-2 -_, 3-(cyclopropylphenylmethyl) -5,6,7,8, 9 -pentahydro-10- (1-methyl-2-hydroxyethyl) (2-methyl-2- Hydroxyethyl) -4-hydroxy-2H-cyclooctyl [b] ftf ran-2-one, 3- (cyclopropylphenylmethyl) -5,6,7,8,9-pentahydro-10- (2-methyl-2-hydroxyethyl) (2-methyl-2-hydroxyethyl) -4-hydroxy; 2H-cyclooctyl L b] nanan-2-pyrene, and cyclopropylcylmethyl ) -5,6,7,8,9-pentahydro--10- (2,3-epoxypropyl) -4-hydroxy-2 fluorene-cyclooctyl [b] piperan-2-one. s 9 · The compound according to item 7 of the patent application scope is selected from the group consisting of the following: 5, β, 7,8,9, 10 -hexahydro-4-hydroxy- 3- (1-benzyl Propyl) -2H-cyclooctyl [blpiperan-2- _, 3- (cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-2 Η -Cyclooctyl [b] fl ditopan-2-one, 3-(: cyclopropylphenyl 1methyl) -6,7,8,9-tetrahydro-4-hydroxy-cycloheptane [b] pipe_ -2 (5 Η)-_, printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs (please read the precautions on the back before filling this page) 3- (dicyclopropylmethyl) -5,6,7, 8,9,10-hexahydro-4-hydroxy-29-cyclooctyl [b] piperan-2 -fluorene, 3- (cyclopropylbenzylmethyl) -4-hydroxy-6,7,8,9 , 10, Ή'-hexahydro-5 Η -cyclooctyl [h] ran-2-one, 9-cyclopropylmethyl-3- (cyclopropyl-benzylmethyl) -4-hydroxyfluorene-6 , 7, -25-This paper size applies to Chinese national standards (CNS> A4 specification (210X297 mm) A8 B8 C8 D8 6. Application scope of patents' 8.9-4-5H -cycloheptane [b] Ninan-2-copper , 9-but-3-enyl- 3- (cyclopropyl-phenylmethyl) -4-hydroxy-6,7,8, 9-tetra'hydro-51 cyclohepta [1]] piran- 2-keto, 10 -Cyclopropylmethyl-3- (cyclopropylphenylmethyl) -4 -hydroxy-5,6,7,8,9,10-hexahydro-cyclooctyl [b] piperan-2 -fluorene , 3-(cyclopropylbenzylmethyl) -1 0 -ethyl-4 -hydroxy-5, 6, _7, 8,9, 10 -hexahydro-cyclooctyl [b] piperan-2- _, 3- (cyclopropyl-¾ylmethyl) -4-hydroxy-10-propyl-5, 6, 7, 8, 9, 1. 〇-hexahydro-cyclooctane [bl pulsan-2-one , 10-Butyl-3- (cyclopropyl-phenylmethyl) -4-hydroxy-5,6,7., 8,9, 10_hexaamino-cyclooctane [h] pulsan-2_copper , 3- (cyclopropyl-benzylmethyl) -4-hydroxy-10- (1-mer, ylpropyl) -5, § ft, 7,8, 9,10-hexahydro-cyclooctyl [h ] Wan-2--2-, 3- (cyclopropyl-phenylmethyl) -4-hydroxy-1 0-isobutyl-5, Γ), 7, 8, 9, 10-hexahydro-cyclooctyl [ h] Chrysan-2-copper, 3- (cyclopropyl-phenylmethyl) -4-hydroxy-10- (3-methylbutyl) -5, δ, 7, H10-hexahydro-cyclooctyl [b] piperan-2-one, and 3- (cyclopropyl-benzylmethyl) -4-hydroxy-10- (tetrahydro-furan-3-ylmethyl) -5,6,7, 8,9,10-hexahydro-cyclooctyl [b] piperan-2-one. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back before filling this page) Paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) 6. The scope of patent application among which is A8 B8 C8 D8 a) CtnH2m + l '. or b) cyclopropyl; wherein R 5 is. a) -x 1-cm Η 2 m -aryl, b) &quot; Xl-CmHzm-Het &gt; c) -Xt-CH = CH-aryl, d) -Xi. -CnH2n-N'HC (0) -〇-CnH5 &gt; n.aS e) -Xi-d…, tM-H et, or g) -X '-C ” H 2 -halogen; printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economics where X 1 is a) -NHS 0 2-&gt; or b)-NHC (0)-; where m is from 0 to 4; where η is from 1. to 4; -27-(Please read the notes on the back before filling this page) This paper size is applicable to China National Standard (CNS) A4 (210 × 297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A8 B8 C8 D8 6. The scope of patent application where P is 3 or 4; where t is 3 or 4 Where aryl is a) phenyl is 0 to 2 substituted, or b) phenyl; where Het is a 5- or 6-membered saturated or unsaturated ring containing from 1 to 3 heteroatoms selected from the following, Includes: nitrogen, oxygen, and fluorene, and includes any bicyclic group in which any heterocyclic ring on the fluorene is fused with a benzene ring or another heterocyclic ring; and is substituted by 0 to 2 Rv; Salt. Π. The compound according to the scope of application for patent, wherein the aryl group is phenyl group; wherein H ft t is a) fluorenyl,, -b) quinolinyl, c) mosothiadiazolyl, d) benzofuryl, e) tellurylphenyl, or, f) pyridyl; where R β is a) methyl, b) ethyl, c) -C1, d)-F »-28-paper Applicable to China National Standard (CNS) A4 specification (210X297 mm) ef— (Please read the precautions on the back before filling this page) Order-A8 B8 C8 D8 々, printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs System 1 e)-B r * f) -I * g) -no2, h) -〇CH3, η -cf3 &gt; j) -CK &gt; k) -C 0 0 H, 1) -N = N- Phenyl, m) -N'H-OH * n) -N (CH3) 2, 0) -NH 2, P) -OCFs, q) -CH2-Br &gt; r) -C (0) NHa &gt; s) -C i 0) 0 CH 3 &gt; t) -OH &gt; u) --NH-S02 \ / (CH2) u V) -CH ^ OH &gt; w) -NH-(CH 2) a-0 H * x) -N ((CH2) 2-〇H) 2, or y) -NHSn2- (CHa) 3-Cl; where R 7 is -29--------- «install-( Please read the notes on the back before filling out this Page) The size of the paper used in the edition is in accordance with Chinese National Standard (CNS) A4 (210X297 mm) A8 B8 C8 D8 々, patent application scope a) methyl, b) -SO 2-phenyl, c) -Cl &gt; d )-B r] e) isomorphazolyl, or f) pyridyl; where-is -Η; where u is 3. 1 2. The compound according to item 10 of the scope of patent application, which is represented by the following formula v〗 I] (please read the precautions on the back before filling this page) -pack. Ordered as a) 3¾ b) cyclopropyl; where R s is a)-X,-aryl, b)-X%-H et, &gt; or c) -Xi-CH (HH-C (0 ) -n-CnHan * i) -CH2-Het; where 5ΰ is a) m-, or -30-This paper size is applicable to China National Standard (CNS) A4 (210X297 mm). &lt;! n Cha. Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, A8 Βδ C8 _ D8 ____ VI. Application scope b)-Η HC (0)-; where m is from 2 to 4; where η Is 4; where aryl is substituted by i 1; where Het is a 5- or 6-membered saturated or unsaturated ring containing 1 to 3 heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur And any bicyclic group including any of the above heterocyclic rings may be fused with a benzene ring or another heterocyclic ring; and substituted with 0 or 1 R 7; and pharmaceutically acceptable salts thereof. 13. The compound according to item 12 of the scope of patent application, which is represented by the following formula I X: Where R is a) aryl, or, b); where aryl is phenyl substituted by 1 R β; where Het is a 5- or 6-membered saturated or unsaturated ring containing from i to 3 selected from The following heteroatoms include nitrogen, oxygen, and sulfur, including any bicyclic group, in which any of the above-heterocyclic rings can be fused with a stupid ring; and 0 or 1 -31-Ϊ paper collision using Chinese national standards ( CNS) A4 · (210x297 public director) '' (Please read the precautions on the back before filling this page) Employees' Cooperatives of the Central Standards Bureau, Ministry of Economic Affairs, A8, B8, C8, D8 6. Replaced by the scope of patent application; and its pharmaceutically acceptable salts. Is a) fluorenyl, b) benzothiadiazolyl c) oxazolyl; wherein R is a) -CN, b) -Cl, c) -F, d) -NΗΠΗ &gt; e) -C (0) NΗ2-f) -C (0) 0 C Η 3 * g) --NH-* SO, \ / (CH2) uh) -HHS0a- (CH2) 3 n -CH2-〇H &gt; §ζ j) -N ((CH; &gt;) 2-Π H) where R π is methyl; where u is 3; and pharmaceutically acceptable salts thereof. 15. According to item 10 of the scope of patent application The compound is selected from the following sisters -32-This paper size applies the Chinese National Standard (CNS) A4g (210X297 cm) (Please read the precautions on the back before filling this page), 1T · A8 B8 C8 D8 The scope of the patent application: N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2-2-cyclooctyl [b] piperazine Alan-3-yl) methyl] phenyl] -benzenesulfonamide K- [3- [cyclopropyl (5,6,7,8, 9, 10-hexahydro- 4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-ethylenesulfonamidoaminocarboxylic acid, [3-[[3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] Amine] -3 -ketopropyl] -1,1-dimethylethyl ester N- [3- [cyclopropyl (5, Γ), 7,8,9,10 -hexahydro-4-hydroxyl -2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-propanesulfonamide N-[3- [cyclopropyl (5,6,7,8 , 9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclodip [b] piperan-3 -yl) methyl] benzyl] -4 -methyl-benzenesulfonamide 1 [ 3- [Cyclopropyl (5,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -Bubutanesulfonamide 4- 氡 -N- [3- [cyclopropyl (5,6,7, 8., 9, 9,10-hexaaza-4-hydroxy-oxy-2H-cyclooctyl [ b] lanan-3-yl) methyl] phenyl] -benzylamine N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-naphthalenesulfonamide printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back first) Fill out this page again) • 3,4-二 氡 -N- [3- [ Cyclopropyl (5, 6, 7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -benzyl Lutetamine, N-[3- [cyclopropyl (5,6, 7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- ) Methyl] cryptyl]-(R) -benzenesulfonylamine (-) N-[3-[cyclopropyl (Γ), 6,7,8,9, 1 0 -hexahydro-4 -hydroxyl -2 -Oxygen-33-The X degree of this paper conforms to the Chinese National Standard (CNS) A4 ^ (210X297 mm) 6. The scope of the patent application-2H-cyclooctyl [b] piperan-3-yl] A Phenyl] phenyl] -2-phenyl-[(E)]-ethylenesulfonamide (+)-[{-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro 4-Hydroxy-2-oxy-2H-cyclooctyl [h] anan-3-yl) methyl] benzyl] -2-phenyl-[(E)]-ethylenesulfonylaminocarboxylic acid, [ 2-[[3-cyclopropyl (5,6,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl] amine]]-2-oxoethyl]-, 1,1-dimethylethyl ester fluorenic acid, [2-[[3-cyclopropyl (5,6,7,8,9 , 10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl] phenyl] amino] -imidazol-4-ylmethyl) -2 -Fluorenylethyl]-, 1,1-dimethylethyl ester [3- [Cyclopropyl (556,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- Fluoro-sulfo-amine · 4-bromo-M-[3-[cyclopropyl (5, (5,7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 2 -cyclo Octyl [bl piperan-3-yl) methyl] phenyl] benzidine_amine Printed by the Consumer Cooperatives of the Central Standardization Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) [3- [cyclopropyl (5, 6, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenylhydrazine] -4-nitro -Benzenesulfonamide H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4 -hydroxy-2-oxy-2 fluorene-cyclooctyl [h] piperan -3 -yl) methyl] cagel] -3 -nitro-cagesulfonamide N- [3-[cyclopropyl (5,6, 7,8, 9,10 -hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [h] anan-3-yl) methyl] phenyl] -4 -methoxy-benzylamine hydrazone- [3- [cyclopropyl (5,6,7 , 8, 9,10 -Hexahydro-4 -hydroxy-2-oxy-34-This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 × 297 cm). 6. Scope of patent application-2H-Cyclo [b ] Piperan-3-yl) methyl] phenyl] -3- (trifluoromethyl) benzenesulfonamide N- [3- [cyclopropyl (5, 6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl] -2,4-difluoro-benzenesulfonamide 3-fluorene-N-[3-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy- 2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-propanesulfonamido-4-cyano-N- [3- [cyclopropyl (5, ( 5,7,8,9,10- $ Hydroxy-4-hydroxy-2-oxy-2H-cyclooctyl.an-3-yl) methyl] phenyl] benzylamine 4-cyano-N- [3- [Cyclopropyl (5, β, 7,8, 9,10-hexahydro-4-hydroxy-2-oxo-2-oxo-cyclooctyl [h] mannan-3-yl) methyl] phenyl ] -¾Luten base salt Η-[3-[Cyclopropyl (5,6,7,8,9,1 0 -Hexahydrodi 4 -hydroxy-2 -oxy-2 Η -cyclooctyl [ h] D Langan-3 -yl) methyl] yl] -8 -Lu-carbon saddle sadic acid, [2-[[3-(R or S): [cyclopropyl (5, 6, 7 , 8, 9, 10) -Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -2-one ethyl ]-, 1,1-Dimethyl ethyl ester The employee's cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs of the People's Republic of China (please read the notes on the back before filling this page) N- [3- [cyclopropyl 6, 7, 8, 9, 10-hexahydro 4-Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,1,3-benzothiadiazole-4 _lutenamine 3- Chloro-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] ane'an-3-yl ) Methyl] benzyl] -sulfenylamine, N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -4-benzofurazolamide-35-This paper is sized to the Chinese National Standard (CNS) A4 (210X297 mm) Ministry of Economic Affairs A8 B8 C8 D8 printed by the Consumers' Cooperative of the Central Bureau of Standards and Administration -2-oxy- 2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide 3-[[[3- [cyclopropyl (5, 6,7, 8 , 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] amino] sulfonyl] -benzylcarboxylic acid (+) -4-chloro-} |-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -benzenesulfonamide (-)-4-chloro-H- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxy-2 -oxy-2H-cyclooctane [ b] Nylan-3-yl) methyl] phenyl] -benzylamine (0-4 -nitro-N- [3- [cyclopropyl (5, Γ), 7,8,9,10 -Hexahydro-4-hydroxy-2 -oxy- 2H-cyclooctyl [b] piperan-3-yl) methyljphenyl] -benzene vine saddle (-)-4-cyano- [cyclopropane (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] BJfan-3-yl) methyl] phenyl] -benzyl Mt [3-[Cyclopropyl (5,6,7,8,9,10-Hexahydro-4 -hydroxy-2 -oxy »:, -2H -cyclooctyl-3-yl) methyl] Cagel] -1-methyl- (SWH-imidazole-4 -sulfofluorene'N- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexahydro-4-hydroxy-2 -Oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl]-4- (phenylsulfonyl) -2 -benzylphenoline_amine N-[3-[cyclo Propyl (5,6,7,8,9,1 0-hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -yl) methyl] benzyl]- 5-(Phenyl. Fluorenyl) -2 -Thienylsulfonamide-3β-This paper size applies to China National Standard (CNS) Α4 size (210X297 mm) (Please read the precautions on the back before filling this page) . 养 • — ^ 1 — ^^ 1 ^ 4: I .... ..... I-I--'n ^ i ·' J VI. Application N- [3- [cyclopropyl (5, 6,7, 8, 9,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3 -yl) Methyl] phenyl] -4 -sulfo-benzenesulfonamide 5-chloro-H- [3- [cyclopropyl (5, 6,7, 8,9,10-hexahydro-4-hydroxy-2- 2- Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-thiophenesulfonamide 4,5-dichloro-N- [3- [cyclopropyl (5,6 , 7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] piperan-yl) methyl] phenyl] -2-thiophenesulfonamide — 4, 5-dibromo-1 [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctane [h] piperan-3- ) Methyl] phenyl] -2-thiophenesulfonate canine cage amine, 4-fluorene-N- [3-[1- (5,6,7,8,9,10-hexahydro-4- Hydroxy-2-oxy-2H-cyclooctyl [b] nanan-3-yl.) Propyl] phenyl] -cylsulfonamide, 4-cyano-N.-[3-[: 1-(5 , (5,7,0-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [Mpiperan-3-yl) propyl] phenyl] -N-[3-[cyclopropyl ( 5, (5, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy, yl -2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4 -Ethyl-toluenesulfonamide-N- [3-[cyclopropyl (5, 6,7,8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclo [b] Piran-3-yl) methyl] benzyl] -4- (phenylazo) -benzenesulfonium_amine Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back first) Fill in this page) (+) -N- [3- [Cyclopropyl (5, 6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Alan-3-yl) methyl] benzyl] -4-oxo-benzylamine (:-)-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro -4-Hydroxy-2-oxo-2 fluorene-cyclooctyl [h] anan-3 -yl) Φ group &quot; 1phenyl] -4 -fluorobenzyl rattan limb &lt; Urethane, [2-「[: WR or S)-[Cyclopropyl (5 f 6, 7, 8, 9, 1 0--3 7-This paper size applies to Chinese National Standard (CNS) A4 Specifications (210X297 mm) A8 B8 C8 D8 6. Application scope of patents hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl '| amine ] -Bu (S)-(1H-imidazol-4-ylmethyl) -2-oneethyl]-, 1,1-Dimethylethyl ester phosphonocarboxylic acid, [2-[[3- (R Or S)-[cyclopropyl (5, 6, 7, 8,9, 10-hexamethyl-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan.-3-yl) methyl ] Phenyl] fluorenyl] -1- (S)-(1H-imidazol-4-ylmethyl) -2-fluorenethyl]-, 1,1-dimethylethyl ester N- [3- [ Cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- Benzylsulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan -3 -yl) methyl] phenyl] -5-(3-isomorphazolyl) -2-thiophenesulfonamine N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10 -Hexahydro-4-hydroxy'-2-oxy-2 hydrazone -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -3 -pyridinesulfonamide Printed by the Bureau of Labor Standards Consumer Cooperatives (please read the notes on the back before filling this page) (〇-N-[3-[cyclopropyl (5,6,7,8 '9,10 -hexahydro-4 -Hydroxy-2 -oxy-2 fluorene -cyclooctyl [h] piperan-3 -yl) methyl] phenyl] -8 -quinoline sulfonamide (-)-N-[3-[cyclopropyl (5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -S- ϋquinoline sulfonamide Η- [3-[cyclopropyl (5, 6,7, 8, 9, 10 -hexahydro-4-hydroxy-2-oxy-2 环 -cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -5- (2-pyridyl) -2-thiophenesulfanyl • N-[3-[cyclopropyl (5, 6,7,8,9,1 0- Hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4- (hydroxylimyl.yl) -benzyl. -38- This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) 6. Scope of patent application. N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxy-2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl]-4- (dimethylamino) -benzenesulfanamide. 3-Amino-N- [ 3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy'yl-2 -Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide, and hydrazone-[3-[cyclopropyl (5,6, 7,8,9 , 10 -Hexahydro-4-hydroxy-2-oxy-2 -cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -4-(trioxymethoxy) -benzyl 4- (bromomethyl) -bu [3- [cyclopropyl (5, (5,7,8,9,10-hexahydro-4-hydroxyl-2-oxy-2H-cyclooctyl [b] Manan-3-yl) methyl] phenyl _]-benzyl_fluorene 4-[[[3- [cyclopropyl (5, β, 7, 8,9, 10 -hexahydro-4 -hydroxy-2 -Oxy-2Η-cyclooctyl [blpiperan-3-yl) methyl] phenyl] amino] shutino] benzene 醢 睽 i:-)-N-[3-[cyclopropyl (5. , 6,7,8, Q, 10 -Hexahydro-4 -hydroxy-2 -oxy-2Η-cyclooct-3-yl) methyl] phenyl] -1-methyl-1Η -Weiji-4 -Lutenamine. Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) Ν- [3- [cyclopropyl Oxy-4 -hydroxy-2 -oxy-2fluorene-cyclooctyl [b] lanan-3-yl) methyl] phenyl] -5- (phenylphenylstable, 1 'S)-2 -phene Sulfonamide N-[3-[cyclopropyl (5, 6,7, δ, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η- Octyl [h] piperan-3 -yl) methyl] phenyl] -5 -methyl-3 -pyridinesulfonate-39-This paper; ^ degrees apply to Chinese national standards (CNS> A4 specifications (210X297 mm) ) A8 B8 C8 D8 VI. Application scope of patents. N- [3- [cyclopropyl. (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- (hydroxyamino) benzylamine 3-[[[3- [cyclopropyl (5, 6,7,8,9, 10 -Hexahydro-4 -hydroxy-2-oxy-2H-cyclooctyl_ [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -methyl benzoate [-[ 3-[Cyclopropyl (5,6, 7,8, Q, 10-hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -3-Hydroxy-sulfenazamide, benzsulfenamide, 4-fluoro-N- [3-Π- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxo -2H-cyclooctyl [b] piperan-3-yl) butyl] phenyl] -N- [3- [cyclopropyl. [3- (2-isothiazolidinyl) phenyl] methyl- (5,6, 7 ,? , 1,10-hexahydro-4-hydroxy-$, $ '-dioxide) Methyl: 1phenyl: 1-3-[(Cagenylsulfonyl) fluorenyl] -4-2 fluorene-ring [b] Piran-2-one-3 -aero-N-[3-[cyclopropyl (5,6,7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -Cyclooctyl [h] piperan-3 -yl) methyl.phenyl] phenyl] -3-[(phenylsulfonyl) amino] -1 -propanesulfonylamine, hydrazone-[3-[cyclopropyl (5, ft, 7, 8,9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan-3-yl) methyl] cage 棊] -3 -[Methanol] -Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) N-[3-[Cyclopropyl (5, β, 7,8 , 9,1 0 -hexahydro-4 -hydroxypoly-2 -oxy_2Η-cyclooctyl [b] piperan_3-yl) methyl] cagel] -3-[(2-ethanol) amino ] -¾ 碕 -amine, and N- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 Η-cyclooctyl [b] Piperan-3 -yl] methyl] phenyl-3-[(bis (2-ethanol) amine-4 0-This paper uses Chinese national standard (CNS) A4 size (210X297 mm) A8 B8 C8 D8 VI. Patent application scope] -benzene Sulfuramine. 1 6 _ The compound of the scope of patent application No. 12 which is selected from the group consisting of: 4-cyano-N- [3-[cyclopropyl (5, 6, 7, 8 , 9,10 -hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -benzenesulfonamide 4-cyano 1- [ 3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -Benzenesulfonamide salt 2- [3-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 Η-cyclooctyl [b ] Piperan-3 -yl) methyl] cyl] -8-quinolinsulfonamide, N- [3- · [cyclopropyl (5, 6,7,8,9, 10-hexahydro-4 -Hydroxy-2-oxy-2 fluorene -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,1,3 -benzothiadiazole-4 -luminol (+) -4 -Chloro-N-[3-[cyclopropyl (5,6,7,8,9, 1 0 -Hexahydro-4 -hydroxy-2-oxy-Z-Cyclotininan_3-Hua ) Methyl] cagel] -benzyl-fluorene (-)-4 -fluorene-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -Hydroxy-2 fluorene -cyclooctyl | [h] ansan-3-yl) methyl] capridyl] -Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the back (Please fill in this page for the matters needing attention) (+)-4-cyano- N- [3- [cyclopropyl (5,6, 7, 8,9,10 -hexahydro-4-hydroxy-2-oxo_ -2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -benzidine (-)-4 -amino-N- [3- [cyclopropyl (5,6,7, 8,9,10 -Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide N-[3-[ring Propyl ('5, 6, 7, S, 9, 1 0 -Hexahydro-4 -hydroxy-2 -oxy ~~ 41-This paper applies Chinese national standard (CNS> A4g (210X297mm) A8 B8 C8 D8 Sixth, the scope of application for patents-2H-cyclooct-3-yl) methyl] phenyl] -bumethyl- (S) -1H-imidazole-4-sulfo-amine, ... (+)-'«-[3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-fluoro-benzenesulfonamide (-)-N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10 -hexahydro-4 -hydroxy-2-oxy-2H-cyclo Octyl [h] manan-3-yl) methyl] phenyl] -4-fluoro-¾pentamine aminocarboxylic acid, [2-[[3- (R or S)-[cyclopropyl (5,6 , 7,8,9,10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino-1-(S)- (1 fluorene-oxazole-4 -ylmethyl) -2 -Pyroethyl]-, 1,1-dimethyl ethyl ester (+) ^-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy- 2Η -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -8 -quinolinesulfonamido (-)-bu [3- [cyclopropyl (5,6,7 , 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -8-pyridinosulfonamide N-[ 3-[Cyclopropyl (5, β, 7,8,9, 1 0-hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [h] piperan-3 -yl) methyl] Phenyl] -4-(Hydroxysalyl) -Benzenesulfonate printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) (5, Γ), 7,8,9 · 1 0 -hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl · phenyl] amino ] Sulfonyl] benzidine (-)-1 [3- [cyclopropyl (5, "), 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl -3-yl) methyl] benzyl] -1-methyl-1H-hoki-4-stilbamine 3-[[[3- [cyclopropyl (5, 7, 8, 9,10-hexa Hydrogen-4-hydroxy-2-oxy-42-This paper size is applicable to China National Sample (CNS &gt; A4g (210X297 cm)) Range-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -methylbenzylsulfonate, 4-fluorenyl-N- [3- [ l- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) butyl] phenyl] -N- [3- [Cyclopropyl [3- (2-isothiazolidinyl) phenyl] methyl- (5,6, 7,8,9,10-hexahydro-4-hydroxy-S, S'-di Oxide) methyl] benzyl] -3-[(phenylsulfonyl) amino]-4 2H -cyclooctyl [b] piperan-2-one 3-chloro-N- [3- [cyclo Propyl (5, Γ), 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -3- [(Phenylpentyl) amino] -1-propanesulfonamide N-[3- [cyclopropyl. (5,6,7,8,9,10-hexahydro-4-hydroxy-2- Oxy-2 fluorene-cyclooctyl [b] mannan-3-yl) methyl] pyridyl] -3- [methanol] -benzylamine, N- [3- [cyclopropyl (5, 6, 7 , 8, 9, 10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] fluorenyl] -3-[(bis- (2-ethanol )) Amine] -benzenesulfonamide 17 · The compound of the 13th scope of the patent application, which is selected from the following ethnic groups: Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read first Note on the back page, please fill in this page) 4 -cyano-N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzylamine 4-cyano-N:-[3- [cyclopropyl (5, 6,7,8,9 , 10-Hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -benzidine sodium nickel N-[3-[cyclo Propyl (5,6. 7 f 8,9,1 0 -Hexahydro-4 -Hydroxy-2 -oxy-4? &Gt;-This paper size applies to Chinese national standards (CNS> A4 size (210X297mm) A8 B8 C8 D8 6. Application scope of patent-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -8-quinolinesulfonamide N- [3- [cyclopropyl (5, 6, 7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,1,3-benzyl Benzothiadiazole-4-glutamate (+)-4-chloro-[cyclopropyl (5, 6,7,8,9,10 -hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (-)-4-oxo-1 [3- [cyclopropyl (5, "), 7,8,9, 10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl] fluorenyl] -benzenesulfonamide (+)-4- -N- [3-[_ cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] nanan-3 -yl ) Methyl] phenyl] -benzenesulfonium W (-)-4-cyano-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-meryl) -2-oxy-2H-cyclooctyl [b] pipe'ran-3-yl) methyl] phenyl] -benzenesulfonyl rattan K-[3-[cyclopropyl (5, Γ), 7,8 , 9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl-3 -yl) methyl] • yl] -methylmethyl- (S)-1 fluorene -midol-4 -sulfo Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the notes on the back before filling this page) (: +)-卜 [3- [cyclopropyl (5,6,74,9,10-hexahydro- 4-hydroxy-2-oxy- 2 氧基 -cyclooctyl [h] anan-3-yl) methyl] benzyl] 4-fluoro-benzylamine (-) 1- [3- [cyclopropyl (5 , 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -4 -fluoro-benzene code Limb (+)-bu [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2H-cyclooctyl [h] piperan-3- Yl) methyl] cryptyl] -8-pyridinosulfonamidin ί-) N- [3- [cyclopropyl (5,6,7, 8, 9,10 -hexahydro-4 -hydroxy-2- Oxygen-44-This paper size applies to China Quasi (CNS) A4 specification (210X297 males) 8 8 8 8 ABCD 6. Patent application scope-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -8-pyridinosulfonyl Amine N- [3- [cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl [Phenyl] -4- (hydroxylamino) -benzenesulfonyl diamine 4-[[[3_ [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxo -.. ,, -2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] amino] sulfonyl] -benzylamine (-)-1 [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooct-3-yl) methyl] phenyl] -1-methyl-1H -imidazole- 4-sulfo saddle 3-[[3-[cyclopropane. (5, β, 7,8,9, 10 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] Piperan-3 -yl) fluorenyl] cagel] amino] sulfofluorenyl] -methyl benzoate N-[3-[cyclopropyl [3-(2 -isothiazolyl) phenyl) methyl -(5,6, -.......-7.H10 -Hexahydro-4-hydroxy-s, s · -dioxide) methyl] phenyl] -3-[(phenylsulfonyl ) Amino]-'4-2 fluorene-cyclooctyl [b] piperan-2 -copper% 3 -fluorene-'N-[3-[cyclopropyl (5, 6, 7, 8, 9, 9 -Hexahydro-4 -hydroxyl -2 -oxy-2H-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -3-[(phenylpenthenyl) amino] -1 -propanesulfonamide Printed by the Consumer Standards Cooperative of the Central Bureau of Standards (please read the notes on the back before filling this page) Η-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxyl -2 -oxy-2 Η -cyclooctyl [b ΐpiperan-3 -yl) methyl] phenyl] -3-[methanol] -benzidine mm-[3-[cyclopropyl (5, 6,7, HI 0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [h 1piperan-3 -yl] methyl] cryl] -3-[(bis- (2- Ethanol) -45-This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm). 6. Scope of patent application) Anthracene] -sulfasulfonamide. (Please read the precautions on the reverse side before filling out this page) 1 3 · The compound according to item 1 of the scope of patent application, which is selected from the group consisting of: 3- (cyclopropylphenylmethyl) -5 , 6,7,8,9,10-hexahydro-4-hydroxy-10- (2-Cyclo-1-methylethyl) -211-cyclooctane [叼 piperan-2-copper 3-(cyclo Propylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy- 1 0-(2 -hydroxypropyl) -2 fluorene -cyclooctyl [b] piran-2 -Keto 3- (cyclopropylbenzylmethyl) -5,6,7,8, 9,10 -hexahydro-4-hydroxy-10- (oxiranylmethyl) -2H -cyclooctyl [ b] piperan-2-one. 3-[(3-aminobenzyl) cyclopropylmethyl] -5, Γ), 7,8,9,10-hexahydro-4- meridyl-2H -Cyclooctyl. [B] mannan-2-fluorenylcarboxylic acid, [3-[[3- [cyclopropyl (4-hydroxyman-2-oxy-2H-benzobenzopiperan-3-yl) Methyl] S group] Amino] -3 -ketopropyl]-, 1, dimethylformamylacetate, [3- [cyclopropyl (4-hydroxy-7-methoxy-2 -Oxy- 2 Η-1-caged piperan-3 -yl ') methyl] phenyl]-, phenylmethyl ester anthracenecarboxylic acid, [3- [[3- [cyclopropyl (4- .Transyl-7-methoxy-2-oxy-2'-pyronopiperan-3-yl) methyl] phenyl] amino] -3-copper Based]-, 1,1,2-dimethylethyl ester Coumarin printed by the Consumer Cooperative of the China Standards Bureau of the Ministry of Economic Affairs, 4-hydroxy-3-(cr-(3-((3-1 Η-indole- 1-yl) -1 -ketopropyl) amino) benzyl) cyclopropylmethyl) coumarin, 4-hydroxy-3- (1-phenylpropyl) -7-propoxy 3- ( Cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-1. 0-[(tetrahydro-2 -furanyl) methyl] -2 fluorene -cyclo Xin [b] Piran-2-嗣 -46-This paper size applies to Chinese national standard (CNS> A4 ^ grid (210X297 mm) 6. Application scope of patent 3- (Cyclopropylbenzylmethyl) -5 , 6,7,8,9,10-hexahydro-4-hydroxy-10-[(tetrahydro-2 -furanyl) methyl] -2 fluorene -cyclooctyl [b] piperan-2-one-3 (Cyclopropylphenylmethyl) -5,6,7, S, 9,10-hexahydro-4-hydroxy-10- [2- (2-methoxyethoxy) ethyl] -2H- Cyclooctyl [b] piperan-2-one 3- (cyclopropylbenzylmethyl) -5,6,7,8,9,10-hexahydro-4 -hydroxyl-1 0-(hydroxymethyl) -2 hydrazone-cyclooctyl [b] piperan-2-fluorene 3- (cyclopropylphenylmethyl) -5,6,7,8, 9, 10-hexahydro-4-hydroxy-10-Π- _Propyl) -2Η-cyclooctyl [b] piperan-2-one 3- (cyclopropylbenzylmethyl) -5,6, 7,8,9,10-hexahydro-4-hydroxy-10-Π-hydroxy-1-methylethyl) -2H-cyclooctyl [b] piperan-2-copper '10- (cyclopropyl via (Methyl) -3- (cyclopropylphenylmethyl) -5, β, 7,8, 9. &quot; 10-hexaoxy-4-Cycium-21 ^ -cyclooctane [1 ^] wool 2 -Copper. 3- (fluorenylpropylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy_10- (methoxycyclomethyl) -2Η-cyclooctane [ b] Huangan-2- 嗣 3- (cyclopropylbenzylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-10- (2-hanyloxyethyl) -2H-Cyclo [b] mairan-2- 嗣 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) 3-(Cyclopropylbenzylmethyl) -5 , β, 7,8,9,1 0 -Hexahydro-4 -hydroxyamidine-10-[(tetrahydro-2′-piperan-3-yl) methyl] -2′-cyclooctyl [h] piperan- 2-copper 3- (cyclopropylcylmethyl) -6,7, «, 9-tetrahydro-4-hydroxy-9- [2-! '2-methoxyethoxy) ethyl] ring Hept [bl piperan-2 (5H) 3- (cyclopropylphenylshenyl) -6,7,8,9-tetrahydro-4-hydroxy-9- [2- [2- (2-methoxy Ethoxy) ethoxy] ethyl] -cycloheptane [called piperan-2 (5 Η)-_ 3-(cyclopropylamidinomethyl) -β, 7,8,9 -tetrahydro- 4-hydroxy-9- (benzyl -47-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 Gongcheng) A8 B8 C8 D8 VI. Patent application scope Methyl) -Cyclopepta [b] Piran-2 (5 Η) -Ketone 3- (Cyclopropylbenzylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (2-methylpropane4) -cycloheptyl [b] piperan-2 (5H) -copper 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- (3-methylbutyl) cyclohepta [b] Nepta-2 (5H)- Ketone 3- (cyclopropylbenzylmethyl) -9-ethyl-6,7,8,9-tetrahydro-4-hydroxy-cyclohepta [b] piperan-2 (5 Η) -one 3- (Cyclopropylphenylmethyl) -9- [2- (1,3-dioxocane-2-yl) ethyl] -β, 7,8,9-tetrahydro-4 -hydroxy-cycloheptane [b] Piran-2 (5Η)-嗣 3- (cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9-[(tetraoxy-2Η- Piperan-3 -yl) methyl] -cycloheptane [b] piperan-2 (5 Η) -one 3- (cyclopropylcylmethyl) -6,7tetraoxy-4-hydroxy-9- Propyl-cycloheptyl [h] piperan-2 (5Η)-嗣 3- (cyclopropylphenylmethyl)-(3, 7, 8,9-tetrahydro-4 -hydroxy-9-[( Tetra-fi;-2 -furanyl) methyl] -cycloheptan [h] nean-2 (5 Η)-嗣, 3-(: cyclopropylphenylmethyl) -6,7,8, .9 -Tetrahydro-4-hydroxy-9-[(tetrahydro-2 fluorene-piperan-2 -yl) methyl] -cycloheptan [b] nanan-2 (5 Η) -copper 3-(: cyclopropyl Phenylmethyl) -β, 7,8,9-tetrahydro-4-hydroxy-9-[(tetramethyl-3-furanyl) methyl] cyclohepta [b] piperan-2 (5Η)-_ Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 3- (cyclopropylbenzylmethyl) -6,7, 8,9-tetrahydro-4-hydroxy grave -9- (2-hydroxypropyl) cyclohepta [b] piperan-2 (5 Η)-嗣 3--(cyclopropylphenylmethylW), 7, 8,9 -tetrahydro-4-hydroxy -9- (methoxyethyl) -cycloheptane [b] Nyran-2 (5H) -copper 3- (cyclopropylJgylmethyl) -Γ), 7, 8, 9-tetrahydro-4- Hydroxy-9- (2-methyl-48-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) ~~ A8 B8 C8 D8 6. Application for patent range oxyethyl) cyclohepta [b] piperazine Nan-2 (5H) -fluorene 9- (cyclopropylhydroxymethyl) -3- (cyclopropylphenylmethyl) -6,7,8,9 -tetrahydro-4-hydroxy-cycloheptane [b ] Piran-2 (5H) -ketofluorenic acid, [3-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -3 -ketopropyl Phenyl]-, 1,1-dimethylethyl ester ΓΗ-indole-1 -propanetamine, N-[3-[cyclopropyl (5,6,7, 8,9,1 0 -hexahydro -4 -Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -carbamic acid, [2-[[3- [cyclopropyl (5, β , 7, 8, 9, 10-hexahydro- 4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -1-(S) -Methyl-2 -ketoethyl]-, 1,1-dimethylethyl ester aminocarboxylic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10- Hexahydro- 4-isochun-2-oxy- 2H-cyclooctyl [h] manan-3-yl) methyl] phenyl] amino] -1-[Π-(S)-[(4 -form Cage group) sulfonyl] -1 fluorene-imidazol-5-yl] methyl 1-2 fluoreneethyl]-, 1,1-dimethylacetamidate aminocarboxylic acid, [2-[[3- [Cyclopropyl (5, β, 7, 8, 9, 10-hexahydro-4-hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] Amine] -2 -Oxyethyl]-, 1,1-Dimethyl ethyl ester Printed by the Consumer Cooperatives of the Central Standardization Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) , [4-[[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-release-2-2-oxy-2 -2-cyclooctyl [b] Alan-3 -yl) methyl] phenyl] amino] -4 -oxobutyl]-, 1,1-dimethyl-ethyl-yl ester, 1 (S) -pyrrolidinecarboxylic acid, 2- [ [[3-[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] Benji-49-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 6. Application scope of patents 1 Amine group] Carbonyl group]-, 1, 1,2-Dimethyl ethyl ester anthryl Formic acid, [2-[[3- [cyclopropyl (5, β, 7,8,9,10-hexahydro- 4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3- (Methyl) phenyl] phenyl] amino] -methyl-2-oxoethyl]-, 1,1-dimethylethyl ester aminocarboxylic acid, [2-[[3- [cyclopropyl (5 , 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan J3-yl) methyl] phenyl] amino] -oxazole-4 -Ylmethyl) -2 -ketoethyl]-, 1,1-dimethylethyl ester hexahydropyridinepropanamine, N- [3- [cyclopropyl (5, β, 7,8, 9, 10-Hexafluorene-4-hydroxy-2-oxamidine-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] benzylamine, 4-ammonia-N- [3- [ Cyclopropyl (5, (5,7,8,9,10-hexahydro- '4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzene ] -N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl ) Methyl] phenyl] -benzylacetamide • N-[3-[cyclopropyl (5, 6, 7, 8, 9 J 0 -hexahydro-4 -hydroxy-2 -oxy-2H-ring Octyl [b] piperan-3-yl) methyl] benzyl] -3-benzyl-2-propenylamine Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling in this card) ) [3- [Cyclopropyl (5, (5,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl Phenyl] -phenyl] -amine-benzylamine, N-[3-[cyclopropyl (5,6,7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2H- Cyclooctyl [b] manan-3-yl) methyl] benzyl.yl] -4 -fluoro-hansamine, N- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexa Hydrogen-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [h] piperan-3 -yl) methyl] phenyl] -50-This paper size applies to China National Standard (CNS) A4 (210X297) Li) 6. Scope of patent application Benzenecarboxamide, N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] benzyl] -carbamic acid, U-[[3- [ Propyl (5 &gt; 6,7,8,9Λ0-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -bu (S)-(1 fluorene-imidazol-4-ylmethyl) -2 -fluoreneethyl]-, 1,: L -dimethylethyl ester aminocarboxylic acid, [3-[[3- [cyclopropyl (2,5,6,7,8,9-hexahydro-4-hydroxy-2-cycloheptyl [b] piperan-3-yl) methyl] phenyl] amino] -3-copperyl ]-, 1,1-Dimethylethyl ester 1 Η-indole-1 -propanamine, N-[3-[cyclopropyl (2,5,, 6,7,8,9 -hexaoxy -4-Hydroxy-2: ketocycloheptan [h] piperan-3-yl) methyl] phenyl]-.. anthanoic acid, [2-[[3- [cyclopropyl (5, β, 7 , 8, 9, 10-Hexahydro-4-hydroxy-2-fluorenyl-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] (phenylenyl) amino] -2 -Oxyethyl]-, 1,1-dimethylethylammonium ammonium acid, [3-[1-(5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy- 2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) propyl] cyl]-, phenylmethyl ester 2H-cyclooctyl [b] piperan-2-fluorene, 3-U -C3-Aminobenzyl) propyl] -5,6 · 7,8,9, 1 () -hexamethylene-4 -hydroxyl-Printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs (please read first Note on the back page, please fill in this page again) fluorenyl Θ acid, [3-f [3- [1- (5, β, 7,8,9, 10-hexahydro-4-hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan-3 -yl) propyl] phenyl] amino] -3 -ketopropyl]-, 1., dimethyldimethylethylpropionamidine, 3-amino -1 [3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2 · * oxy-2H-cyclooctyl [blfiiSan-3-yl) propyl] benzene Base]-, monohydrochloride ~ 51-This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 6. Application scope of patents Sulfuramide, 4-chloro-N-[3-[: 1 -(5,6,7,8,9,10-Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) propyl] phenyl] -cage Sulfo_amine, 4-chloro-N- [3- [l-(! 3,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Piperan-3-yl) propyl] phenyl] -N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H- Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N'-ethylurea N- [3- [cyclopropyl (5,6,7,8,9, 10-hexahydro- 4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N · -phenyladeno [3-[cyclopropyl (5, Γ), 7, 8, 9, 10 -hexahydro-4- Hydroxy-2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl]-, phenyl ester aminocarboxylic acid r [3- [cyclopropyl (5, β, 7, 8,9, 10-Hexahydro-4-hydroxy-2-oxy-2H -cyclooctyl [b] pyran-3 -yl) methyl] phenyl]-, ethyl ester. Limyl formic acid 2 Η- Cyclooctyl [b] piperan-2-_, 5, β, 7,8,9,1 0 -Hexahydro-4 -hydroxy-3-(2-methyl-1 -fluorenylpropyl)-(+ )-(!?)-3- (cyclopropylrongylmethyl) -5,6,7,8,9,10-hexahydro-4 -hydroxy-2--cyclo [b] piperan-2-嗣 (-)-(S) -3- (cyclopropylphenylmethyl)-. 5, β, 7,8, 9,10 -hexahydro-4-hydroxy-2Η-cyclo [b] piperan- Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs of 2-Ketone (Please read the precautions on the back before filling out this page) (R or S) -3- (Cyclopropylcrylmethyl) -6, 7, 8 , 9-tetrahydro-4-hydroxy-cycloheptan [b] piperan-2 (5Η) -one (R or S) -3- (cyclopropylphenylmethyl) -β, 7,8,9 -Tetrahydro-4-hydroxy-cycloheptane [bl piperan-2 (5Η) -copper 3-U)-(cyclopropyl <cyl group] -4 -hydroxy-1 0-(R and S) -propyl base- 5. R f 7 U ， 1 0 -Hexahydro-cyclooctane [b] Piran-2-嗣 -52-This paper size is applicable to Chinese National Standard (CNS) A4 Washing (210X297 male) A8 B8 C8 D8 Sixth, the scope of application for patents 3- (R) _ (cyclopropyl cage methyl) -4-hydroxy-10- (R or S) -propyl-5. 6,7,8,9,10-hexahydro -Cyclooctyl [b] nesan-2- 嗣 ^ 3-(R) -cyclopropylcylmethyl) -4 -hydroxy-1 0-(R or S) -propyl-5, 6, 7,8 , 9,10-hexahydro-cyclooctyl [b] nanan-2-one 3- (S)-(cyclopropylphenylmethyl) -4 -hydroxy-10-U and S) -propyl-5 · β, 7,8,9,1 0 -Hexahydro-cyclooctyl [b] piperan-2-one-3 (S)-(cyclopropylphenylmethyl) -4-hydroxy-10- (R or S) -propyl-5, 6, 7, 8, 9, 10-hexahydro-cyclooctyl [b] piperan-2- 嗣 3- (S)-(cyclopropylphenylmethyl) -4- Hydroxy-10- (R or S) -propyl-5. Β, 7,8,9,1 0-hexahydro-cyclooctyl [b] piperan-2-ketoanthanoic acid, [2-[[3 -(R or S)-[cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 2-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] fluorenyl] -2-ketoethyl]-, 1,1-dimethylethyl ester Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the note on the back first) Matters need to be filled out on this page) Urethane, [2-[[3-(R or S)-[Cyclopropyl (5, β, 7, 8, 9, 1 0) -Hexa-4-hydroxy-2 -Oxy- 2Η-cyclooctyl [b] piperan-3-yl) methyl]. Benzoj warm roll] -2-_ethyl]-, 1,1-di.methyl ethyl ester Γ 垵Carboxylic acid, [2-[[3- (R or S)-[cyclopropyl (5, β, 7,8,9.10-hexahydro-4 -hydroxy-2 -oxy-2 -2-cyclooctyl [h ] Piperan-3 -yl) hamyl] cagel] fluorenylfluorene-1-(S)-Πfluorene -oxazole-4 -ylmethyl) -2 -ketoethyl]-, 1, 1 -di Methyl Ethyl Ester Acrylate '[2-[[3- (R or S)-[Cyclopropyl (5,6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] imidazol-4-ylmethyl) -2-ketoethyl]-, 1,1-dimethylethyl Ester-53-This paper size applies to Chinese National Standards (CNS> M Specification (2! 0X297 cm) A8 B8 C8 D8 6. Application for Patent Range 3- [Cyclopropyl- [3- (phenylmethyl) amino] Phenyl] methyl] -5,6, 7, 8, 9, 10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperan-2-one, 3- [cyclopropyl- [3- [(2-phenylethyl) amino] phenyl] methyl] -5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2H-cyclooctyl [b] piperazine Hexan-2- 嗣 H- [3- [cyclopropyl (5, 6, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3 -Yl) methyl] phenyl] -N- (benzyl) -bentrozamine N- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexahydro-4-hydroxyl -2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N- (benzylmethyl)-'methanesulfonamide "3- [cyclopropyl (5 , 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N- (2-benzene Ethyl) -sulfosulfenylamine (-)-3-[(3-aminephenyl) cyclopropylmethyl] -5, (5,7,8,9,10-hexahydro-4 -hydroxy- 2H-cyclooctyl [b] piperan-2-hydrazone; and (+)-3-[(3 "aminophenyl) cyclopropylmethyl] -5, 6,7, 8, 9, 10 -hexahydro 4-Hydroxy-2H-cyclooctyl [b] piperan-2-one-3- [cyclopropyl- [3-amino] phenyl] methyl] -5,6,7, 8, 9, 10 -Hexahydro-4-jingyl-2H -Cyclo [h] piperan-2-Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) (+)-3 -[Cyclopropyl- [3 -amino] -5, β, 7,8, 9, 10-hexahydro-4-hydroxy-2 羟基 -cyclooctyl [b] piperan-2-嗣 (-)- 4 -Ga-N-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0-Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [h] piperan-3 -yl) methyl] benzyl] -cylsulfonamide (+)-4 -gas-N- [3-[Cyclopropyl (5, Γ), 7, 8,9, 1 0 -Hexahydro-4 -hydroxyl_ -54 _ This paper size applies to China National Standard (CNS) A4 specification (210X297 mm) Αδ Β8 C8 D8 6. Application scope of patents 2-oxy-2H-cyclooctyl [1] piperan-3-yl) methyl] phenyl] -benzenesulfonamide 3- [cyclopropyl (.5, 6,7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4 -fluoro-benzenesulfonium Amine (+) 4- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- ) Methyl] benzyl] -4-fluoro-benzenesulfonamide, (-)-N- [3- [cyclopropyl (5, "), 7,8,9,10-hexahydro-4- Hydroxy-2-oxy-2 fluorene-cyclooctyl-3 -yl) methyl] benzyl] -1 -methyl-1 fluorene-imidazole-4 -sulfonylamine (-)-4-cyano-M -[3-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 2-cyclooctyl [b] nanan-3-yl) methyl] benzene Phenyl] -benzyl saddle (-)-N-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -ring Octyl [h] piperan-3 -yl Methyl] phenyl] -8-quinolinesulfonamide, (:-)-bu [3- [cyclopropyl (5, (5,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -2 -phenyl-[(E)]-vinylpyridine (-)-N-[3- [Cyclopropyl (5, β, 7,8,9,10-Hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3 -yl) methyl] 'benzene Base] -benzenesulfonate_Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 〇) -4-cyano 1- [3- [cyclopropyl (5,6 , 7,8,9,10-hexahydro-4-hydroxy-2-oxy-cyclooctyl [h] manan-3-yl) methyl] benzyl] -benzylamine (+)-N-[ 3-[cyclopropyl (5, fi, 7,8,9,10-hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] cage ] -8-B quinolinesulfonamide (+)-N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-5 5 -This paper size applies to Chinese National Standard (CNS) A4 specification (210 × 297 mm) A8 B8 C8 D8 6. Application for patent scope Base-2H -cyclooctyl [b] piperan-3-yl) methyl] benzyl]- 2-phenyl-[(E)]-ethylenesulfonylamine 4-cyano-N- [ 3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl ] -Benzenesulfonamide H- [3-[cyclopropyl (5, β, 7, 8, 9,10 -hexahydro-4-hydroxy-2-oxy-2 fluorene -cyclooctyl [b] piperan -3 -Methyl) methyl] benzyl] -8 -quinolinesulfonamide 4 -fluorene-N- [3- [cyclopropyl (5,6,7,8,9, 10 -hexahydro-4- Hydroxy-oxy- 2H-cyclooctyl [h] B} §an-3-yl) methyl] benzyl] -benzene code N- [3- [cyclopropyl (5,6, 7,8, 9,10 -hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b 1piperan-3 -yl] methyl] phenyl] -4-(1,1-dimethylethyl ) -Colinamine 'N-[3-[cyclopropyl (5, Γ), 7, 8, 9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 羟基 -cyclooctyl [b ] Piperan-3 -yl) methyl] phenyl] -2 -naphthosulfonamide H- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexahydro-4-hydroxy- 2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- (trifluoromethyl) -benzonamine N-[3-[cyclopropyl (5 , 6,7,8,9,1 0-Hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b) Pranan-3-yl) methyl] phenyl] -4_gas-benzene δ Huangteng printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please Please read the precautions on the back before filling this page) 3.4 -Dihydrazone- Ν- [3- [cyclopropyl (5, 6, 7, 8, 9, 10 -hexahydro-4-hydroxy-2-oxy- 2Η-cyclooctyl [b] mannan-3-yl) methyl] benzyl] -cage code_limb N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro- 4 -Hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -naphthosulfonium ammonium 2.5 -diazepine-N- [3- [cyclopropyl (5,6,7,8,9,10-Hexahydro.-4-hydroxy-2 -Hydroxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -sulfonium Amine-5 6-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 6. Application scope of patents, 4-bromo-N- [3- [cyclopropyl (5,6, 7, 8,9,10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] BJSan-3-yl) methyl] phenyl] -benzylamine N- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- 4-nitro-benzenesulfonamide N- [3-l: cyclopropyl (5, 6, 7,8, 9, 10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b ] Piperan-3-yl) methyl] phenyl] -3-nitro-benzenesulfonamide-N- [3- [cyclopropyl (5, Γ), 7,8,9,10 -hexagon 4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperidin-3-yl) methyl] phenyl] -4-methoxy-benzenesulfonamide 4-[[[3- [cyclo Propyl (5, Γ), 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl1phenyl] amino ] Sulfo-yl] -benzoic acid N- [3- [cyclopropyl (5,6; 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2Η-Η-cyclooctyl [b ] Nesan-3-yl) methyl] phenyl] -2,4,6-trimethyl-benzazamine hydrazone-[3-[cyclopropyl (5, β, 7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] cyl] -2,3,4,5, β-pentafluoro-¾sulfonyl_ Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Amine Economy (please read the precautions on the back before filling this page) Η- [3- [cyclopropyl (5fr), 7, 8, .9, 10-hexahydro- 4-Hydroxy-2-oxy-2 H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,4-difluoro-benzylsulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] cyl] -3- ( Trifluoromethyl) -benzene code rattan-5 7-This paper size applies to China National Standard (CNS) A4 (210X297 mm) 6. Scope of patent application N- [3- [cyclopropyl (5, 6, 7,8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [h] piperan-3-yl) methyl ] Phenyl] -2-fluoro-benzenesulfonamide 4 -butoxy- N- [3- [cyclopropyl (5,6,7,8, 9, 10 -hexahydro-4 -hydroxy-2- Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] eyenan-3-yl) methyl] phenyl] -5- (dimethylamino) -1-naphthylsulfonium_amine 3 , 5 -Difluorene-h 丨-[3-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 Η-cyclooctyl [b] piperazine Alan-3 -yl) methyl] phenyl] -2 -hydroxybenzylidene 2,3-diazepine-N-[. 3-[cyclopropyl (5, β, 7,8,9,1 0 -'Hexa'hydro-4 -hydroxy-2-oxy-2 fluorene-.cyclooctyl | _b] mannan-3-yl) methyl] phenyl] -benzylcarboxyl N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-meryl-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2- (Trifluoromethyl) -sulfenylamine 2-fluorene-N- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2- 2-oxy-2 Η-cyclooctyl [h] inan-3-yl) methyl ·] phenyl] -6-methyl-benzylum Printed by the Consumer Standards Cooperative of the Ministry of Standards of the People's Republic of China (Please read the precautions on the back before filling out this page) .. 5-二 氡 -Η-[3-[cyclopropyl (5, ft, 7, 8, 9, 1 0-Hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] mannan-3-yl) methyl] $ yl] -bensulfonylamine 3 -fluorene- [3- [cyclopropyl ( 5, 6,7,8, 9,10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] anan-3-yl) methyl] cyl] -benzyl_ 了 Η -[3-[Cyclopropyl (5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl Base] phenyl] -4 -phenylhydrazone_amine-58-This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 6. Application scope of patent 3-Bromo-H- [3- [Fluorenyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2Η-cyclooctyl [b] nickan-3-yl) methyl] phenyl]- Benzylamine 3-[[[3- [cyclopropyl (5, Γ), 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan -3-yl) methyl] phenyl] amino] sulfofluorenyl] -benzoic acid 2 -fluorene-N- [3- [cyclopropyl (5, (5,7,8,9, 10 -hexahydro 4-Hydroxy-2-oxo-2 hydrazone-cyclooctyl [b] piperan-3-yl) methyl] benzene ] -Benzenesulfonium_amine 5 -chloro-N- [3- [cyclopropyl (5, 6,7, 8, 9,10 -hexahydro-4-hydroxy- 2-oxy-2 fluorene -cyclooctyl [ b] piperan-3 -yl) methyl] phenyl] -1, 3 -dimethyl-1 fluorene-pyrazole-4 -fluorene_amine 2. β-diazepine-N-[3-[cyclopropyl (5, "), 7, 8, 9, 10-hexahydro-4 -hydroxy-2-oxoline-2'-cyclooctyl [blpiperan-3-yl] methyl] cyl] -cage Hydrazine N-[[5-[[3-[cyclopropyl (5, Γ), 7,0 -hexahydro-4 -meryl-2 -oxy-2H -cyclooctyl [b] piperan- 3 -yl) methyl] phenyl] amino] sulfonyl] -2 -thienyl 1methyl] -benzyl saddle H- "3- [cyclopropyl (5, 6, 7, 8, 9 ,, 10-Hexahydro-4-hydroxy-2-oxy-2H-cyclooct-3-yl) methyl] phenyl] -1-methyl'yl- (S) -1H-hoe beer-4-code_amine Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) .N- [3- [cyclopropyl (5,6,7, 8,9, 10-hexahydro-4 -Ethyl-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] cryl] -4- (benzylsulfonamide) -2 -thienylsulfonium-amine N- [3 -[Cyclopropyl (5,6, 7,8, 9, 10-Hexa-4--4-yl-2-oxy-2 Η -cyclooctyl [b] piperan-3 -yl) methyl] cage Base) -5-(cage base Amine)-2-phenphenantamine-5 9-This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) 6. Scope of patent application • N- [3- [cyclopropyl (5,6 , 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy / -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-iodo-benzenesulfonium Amine 5 -fluorene-N-[3-[cyclopropyl (5,6,7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [h] piperan- 3-yl) methyl] phenyl] -2-thiophenesulfonamide 4,5-diaza-^-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4 -Hydroxy-2_oxy-2 hydrazone-cyclooctyl [b] piperan-3-yl) methyl] benzenechae] -2-thiophenesulfonium 4,5-dibromo-H- [3- [cyclo Propyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -2- Thiophenesulfonate limbs. 2,5-Diazepine-N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3-thiophenesulfonamide 2.4 -difluorene-fluorene-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -Hexahydro-4 -Ethyl-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] benzidine] -benzyl sulfonamide \ 2,4.6-triamidine-N- [3- [Cyclopropyl (5 , β, 7,8, 9,10 -Hexahydro-4-hydroxy-dain-2 -chloromother-2 Η -cyclooctyl [h 1pipe_-3 -ylpyridyl] cagel] -clamidine m Printed by the Employees' Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling this page). [4-[[[3- [cyclopropyl (5,6,7,8,9,10- Hexahydro-4-hydroxy-2-oxo- 2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] fluorenol 棊] Cagel] '• Ethylpyridine-[ 3- [cyclopropyl (5, ft, 7, 8,9.10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- 4- (phenylazo) -sulfasulfonamide-6 0-This paper size applies to the Chinese National Standard (CNS) A4 specification (210X297 mm) 6. Scope of patent application N- [3- [cyclopropyl ( 5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-[[4 -(Dimethylamino) phenyl] azo] benzenesulfonamide H- [3- [cyclopropyl (5,6,7, 8, 9,10-hexahydro-4-hydroxy-2-oxy -2 fluorene-cyclooctyl_ [b] piperan-3 -yl) methyl] phenyl] -5-(2-pyridyl) -2 -thiophenesulfonamide • 3 -Amosphere-H- [3- [Cyclopropyl (5,6,7,8,9,10-Hexahydro-4-hydroxy- 2-oxy-2H-cyclooctane [b] Uran-3-yl) methyl] phenyl] -2-methyl-benzenesulfonylamine N- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxyl -2-oxy-2 -cyclooctyl [b] piperan-3 -yl) methyl] cryl] -4-(trifluoromethoxy) -benzenesulfenylamine 3 -fluorene- [3- [cyclo Propyl (5, "), 7, 8,9,10 -hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3 -[(Benzyl sulfonated stuffed roll) Saddle] -1 -Propyl β melamine 'N- [3- [Cyclopropyl (5, β, 7, 8,9, 10 -Hexahydro-4-hydroxy- 2-oxy-2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3-piperazine printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the note on the back first) Please fill in this page again) N-[3-[Cyclopropyl (Γ), 6,7, S, 9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2H -cyclooctyl [h] piperazine Nan-3-yl) methyl] phenyl] -5 -methyl-3-pyridinesulfonyl-N- "3- [cyclopropyl (5, fi, 7,8,9,10-hexahydro-4 -Hydroxy-2-oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl1cyl] -ethylenesulfonamide, N-[3-[cyclopropyl (5, β, 7 , 8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxo ^ -2Η -cyclohexyl [h] piperan-3-yl) methyl] 'k group] -form Sulfur_Saddle-61-This paper size applies Chinese National Standard (CNS) A4g (210X297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A8 B8 C8 D8 VI. Application for patent scope. (5, 6, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -ethanesulfonyl醯 睃 N- [3- [cyclopropyl (5,6,7,8., 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl] -benzenesulfonylamine N- [3- [cyclopropyl (5,6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-phenyl-ethylenesulfonylamine N- [3- [cyclopropyl (5,6,7,8,9,10 -hexahydro -4-Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzylsulfonium_amine 1 [5-[[[3- [cyclopropyl ( 5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] limyl] sulfonyl ] -4 -methyl roll-2-peak benzyl] -ethyl_amine N- [3- [cyclopropyl (5, (5,7,8,9,10-hexahydro-4-hydroxy-2-oxo Yl-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2 -g phensulfonamide N-[3-[cyclopropyl (5,6,7,8,9 , 1 0 -hexaaza- 4 -Hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] B-Cetan-3 -yl) methyl] phenyl] -propanesulfonamide N-[3-[cyclopropyl (5, 6 , 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -4 -methyl-benzene Sulfonamide N- [3- [cyclopropyl (5, β, 7,8,9, 10 -hexahydro-4-hydroxy-2-oxy-2 羟基 -cyclooctyl [b] piperan-3- ) Methyl] phenyl] -butanesulfonamide N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4 -hydroxy-2-oxy-2H -Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1,3-dihydro-1,3-difluorene-2 Η -isoindole-2 -ethanesulfonylamine η [ 3- [Cyclopropyl (54,7, 8,9, 10 -Hexahydro-4-hydroxy-2 -oxy-6 2-This paper is compliant with China National Standard (CNS) Α4 ^ grid (210X297 mm) ) -----_----- ^-(Please read the precautions on the back before filling out this page), tT Μ .. 6. Application for patent scope -2H-Cyclo [b] Piran- 3-yl) methyl] phenyl] -2-propanesulfonamide N- [3- [cyclopropyl (5,6,7, 8, 9,10 -hexahydro-4-hydroxy-2-oxy ........ -2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,6-dimethylbenzenesulfonamide N- [3- [cyclopropyl (5 , 6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy-2K-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -2-methylbenzenesulfonate Hydrazine 3-fluorene-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2 hydrazone-cyclooctyl [b] piperan -3 -yl) methyl] phenyl]-: 1-propanesulfonamide &quot; N-[3-[cyclopropyl (5,6,7,8,9,1 0 -hexahydro-4 -hydroxyl -2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -3, 5-bis (trifluoromethyl) -benzyl-amine N- [3- [ Cyclopropyl (5, 6,7, 8,9, 10 -Hexahydro-4-hydroxyfluorenedi 2-oxo-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- 7, 7-dimethyl-2-oxy-bicyclo [2.2.1] heptane-butanesulfonamide sulfonium- [3- [cyclopropyl (5, 6, 7,8,9,10- Hexahydro-4-hydroxy-2-oxy-2 hydrazone-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2, β-dimethoxybenzenesulfonyl S Printed by the Consumer Bureau of Standards Bureau (please read the precautions on the back before filling this page) Η-[3-[cyclopropyl ('5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxyl -2 -oxy-2'-cyclooctyl [h] piperan-3-yl ') methyl] phenyl] -3,4-dimethoxy-benzenesulfonylamine N-[3-[cyclopropyl (5, β, 7,8,9,1 0-hexahydro-4 -hydroxy "'2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- Methyl-toluenesulfonamide 2-bromo-N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2-'t oxo-2 2- Cyclooctyl [h] mannan-3-yl) methyl] benzyl] -β-methoxy-benzyl-R3-This paper uses China National Standard (CNS) A4 (210 × 297 mm) 8 8 8 8 ABCD VI. Patent Application Code: Fujin Saddle H- [3- [cyclopropyl (5,6,7, S, 9,10-hexahydro-4-hydroxy-2-oxy-2 Η-cyclooctyl [h ] Piperan-3-yl) methyl] phenyl] -3,5-dimethyl-4-isomorphazolesulfonamide 2 -cyano-N- [3- [cyclopropyl (5, Γ) , 7,8,9,10 -Hexahydro-4-hydroxydi-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide «-[3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2,1,3 -benzothiadiazole-4 -lucetamine H- [3- [cyclopropyl (5,6, 7,8,9,10-hexahydro-4-hydroxy-2-oxyl Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the notes on the back before filling this page ). -2 Η -cyclooctyl [h] piperan-3 -yl) methyl] benzene 荖] -4 -Ethyl-cylsulfonamide 3- [cyclopropyl (5, β, 7, 8 ,, ' 9, 10 -Hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -4 -propyl-benzenesulfonamide 'N-[ 3-[Cyclopropyl (5, β, 7, 8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -yl) methyl] Phenyl] -1 -octanesulfonamide hydrazone-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclo Octyl [b] piperan-3 -yl ') methyl] benzyl] -1 -dodecanesulfonylamine N-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -4-U -methylethyl) -sulfenyl_amine N -[3-[Cyclopropyl (5, β, 7, 8, 9, 9, 10-hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl ] 笼 基] -benzylsulfonamide H- [3- [cyclopropyl (5, Γ), 7,8,9, 10 -hexahydro-4-hydroxy-2-oxy-2 -2 -cyclo Octyl [b] piperan-3 -yl) methyl] cagel] -5-(3 -isoxazolyl)--64-This paper size applies to China National Standard (CNS) A4 (210X 297 (%) 6. Scope of patent application: 2-thiophenesulfonamide-amino- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctane [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide N-[3- [cyclopropyl (5, 6, 7, 8, 9, 9) 0-hexahydro-4 -hydroxyl -2 -Oxygen ......... -2 Η -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -4-(hydroxyamino) -benzyl-amine H -[3-[cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 Η -cyclooctyl [b] piperan-3 -yl) methyl ] Benzyl] -4-[(Cagenylsulfonyl) Amine] -Cagelinamine, N- [3- [Cyclopropyl (5, β, 7,8,9,10-hexahydro-4 -Hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -3-[(benzylsulfonyl) anthracene] -cylsulfonamide N-[ 3-[[3-[cyclopropyl (5, β, 7,8,9,10 -hexahydro-4 -hydroxy-2 -oxy-2- -cyclooctyl [h] piperan-3-yl ) Methyl] phenyl] amino] sulfofluorenyl] fluorenyl] -benzyl-amine N-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxyl -2 -Oxy-2 hydrazone -cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -4-(dimethylamino) -benzene confirmed the consumption of employees of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the cooperative (Read the notes on the back of the poem before filling out this page) '' 3 -Amine-Η- [3- [Cyclopropyl (5, β ,. 7, 8,9,10 -hexaoxy-4- Carboxyl-2-oxy-21ί-cyclooctyl [b] lanan-3-yl) methyl] phenyl] -3S does have N- [3- [cyclopropyl (5, β, 7, 8 , 9, 10-Hexa-4-hydroxy-2-oxy-2 hydrazone-cyclooctyl [h] piperan-3-yl) methyl1phenyl] -3-(hydroxylamino) -benzylsulfonyl 3-[[[3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-6-6-This paper size applies to Chinese National Standard (CNS) A4 Specifications (210X297 mm) 6. Scope of patent application -2 Η -cyclooctyl [b] nanan-3 -yl) methyl] phenyl] amino] sulfonylamine] -benzoic acid, methyl ester XN- [3- [Cyclopropyl (5, 6,7, S, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl]- 3-[(2-ethanol) amino] -benzenesulfonamide [3- [cyclopropyl (5, 6, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2H -Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- [bis- (2-ethanol)) amino] -benzenesulfenylamine N- [3- [cyclopropyl (5 , β, 7,8,9,10 -hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl] benzene Yl] -3-[methanol] -benzenesulfonylmethane [3-[cyclopropyl [3-(2-isothiopyridyl) benzyl] methyl- (5, β, \ .. 7, 8 , 9,1 0 -Hexahydro-4 -hydroxy-S, S '-dioxide) methyl] phenyl] -3-[(phenylphosphonium) amino] -4-2 fluorene -cyclooctyl [b] Piran-2-嗣 N-[3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2-2-cyclooctyl ] Piran-3-yl) methyl] phenyl] -3- (2-methoxyethoxymethoxy) -benzyl sulfide_amine Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read first Note on the back page, please fill in this page again) Η-[3-[Cyclopropyl (5, β, 7,8,9,1 0 -Hexahydro-4 -hydroxyG -oxy-2 Η -cyclooctyl [b ] Piperan-3 -yl) methyl] cryptyl] -3 -hydroxy-benzylsulfonamide N-[3-[cyclopropyl (5, (5, 7, 8, 9,1 0 -hexahydro- 4 -Hydroxy-2 -oxy-2H -cyclooctyl [b] piperan-3-yl) formamidine] phenyl] -3- (4-morpholinoethoxy) -benzenesulfonamide, N- [3-[Cyclopropyl (5, β, 7,8,9,1 0-Hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -yl) methyl ] 笼 基] -3-(Ν, Κ-diethylamine basic paper size applicable Chinese National Standard (CNS) A4 Specification (210X297 mm) 6. Application for Patent Range Ethoxy) _Benzylamine N- [3- [Cyclopropyl (5, Γ), 7,8,9, 10- Hexahydro-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -4-mesityl-jasmonylamine N- [3- [cyclo Propyl (2,5, β, 7,8,9-hexahydro-4-hydroxy-2-fluorenecyclohepta [b 1anan-3 -yl) methyl] phenyl] -vinylsulfonamide'N -[3-[Cyclopropyl (2,5,6,7, S, 9-hexahydro-4 -hydroxy-2-ketocyclohepta [b] piperan-3 -yl) methyl] phenyl]- Methanesulfonamide N-[3-[cyclopropyl (2,5, (5,7,8,9-hexahydro-4 -hydroxy-2 -fluorancycloheptyl [b] piperan-3 -yl) methyl Yl] phenyl] -ethanefluorenamine-tellurium gadolinium, [3]-[cyclopropyl, (5, 6, 7, 8, 9, 9, 10-hexahydro-4 -hydroxy-2 -oxyl -2 Η -cyclooctane. [H] piperan-3 -yl) methyl] phenyl] -H -phenyl-thiourea, H- [3- [cyclopropyl (5,6,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N-ethyl-¾ethanethio_amine, N -[3- [Cyclopropyl (; 5, β, 7,8,9,10-Hexahydro-4 via per-2-oxo-2H-cyclooctyl i_b] nanan-3-yl) methyl] Phenyl] -5, 6,7,8,9,10-hexahydro-4-hydroxy-3- (1-phenylbutyl) -21 ^ -cyclooctane [h] piperan-2-_ Consumer Cooperatives, Central Bureau of Standards, Ministry of Economic Affairs Yince (please read the precautions on the back before filling this page) "3-Π-(5, β, 7.8, 9, 1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 Η -ring Octyl [b] piperan-3 -yl) -2-methylpropyl] phenyl] -aminocarboxylic acid, phenyl methyl ester 3- "1- (3-aminocyl) -2-methylpropyl Group) -5, R, 7,8,9,1 0 -Hexyl, -4 -hydroxy-2 fluorene -cyclooctyl [b] piperan-2-_ 4 -cyano-N-[3-[1 -(β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan-3 -yl) -2-methylpropyl] phenyl ]-Cages dipped amine-f &gt; 7-This paper size is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 6. Application scope \ 4-\-卜卜 [3- [卜 （ 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) -2-methylpropyl] phenyl] -benzenesulfonate Glutamine only-[3- [Bu (5,6,7,8,9,10-hexahydro-4- meridyl-2-oxy-211-cyclooctyl [b] piperan-3 -yl)- 2 -methylpropyl] phenyl] -1 -methyl-〗-fluorene -footazole-4- [3- [Bu (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 [1-cyclooctyl [b] piperan-3 -yl) butyl ] Phenyl] -aminocarboxylic acid, phenylmethyl ester 3-[1-(3 -fluorenylbenzyl) butyl] -5, β, 7, S, 9,1 0 -hexahydro-4- -2 hydrazone-cyclooctyl [b] lan-2 -coopersulfonyl sulfonamide, 4-ammonia-N-[3-[1-(5, β, 7,8,9,1 0 -hexahydro- 4 -Hydroxy-2 -Syl-2 fluorene -cyclooctyl [b] piperan-3 -yl) butyl] cyl] -benzylamine, 4-cyano-N-[3-[1-( 5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) butyl] phenyl] -3- ( σ-cyclopropylthiophen-2-ylmethyl) -4 -hydroxy-5,6,7,8,9,1 0 -hexahydrocyclooctyl [b] piperan-2-嗣. 3-(«- Ethylthiophene-2-ylmethyl) -4 -hydroxy-5,6,7,, 8,9,1 0 -Hexahydrocyclooctyl [b] piperan-2- 詷 3-(«-ethyl (5-methylthiophene-2-ylmethyl) -4 -hydroxy-5,6,7,8.9,10-hexahydrocyclooctane [b] Piran-2-嗣 Employees of Central Standards Bureau, Ministry of Economic Affairs Printed by the Consumer Cooperative (please read the precautions on the back before filling out this page) 3- (σ -ethylpyrido [b] thiophen-2-ylmethyl) -4 -hydroxyl -5, β, 7,8,9,1 0 -Hexahydrocyclooctyl [b] piperan-2 -copper 3-(«-cyclopropyl (5-methylolfuran-2-yl)- 4-hydroxy-5, B, 7 f 8,9,1 0 -hexahydrocyclooctyl [b 1piperan-2 -copper 3-(«-cyclopropyl (5-hydroxymethylfluoren-2-yl) Methyl) -4 -hydroxyl-6 8-This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) 6. Application for patent scope 5,6,7,8,9,10-Hexacyclic [b] Piran-2- 嗣 3-(«-cyclopropyl (5-(2-hydroxyethyl) thiophene-2-ylmethyl) -4 -hydroxy-5.fi, 7,8,9 , 10-hexahydrocyclooctyl [h] manan-2-one 3-U-cyclopropyl (5- (2-hydroxymethyl (methoxymethyl ether) furanmethyl-2-yl) -4 -hydroxy -5, β, 7,8,9, 10 -Hexahydrocyclooctyl [b] piperan-2-one 3- («-cyclopropyl (5-(2-hydroxymethyl (methoxymethyl ether ) Thiophen-2-ylmethyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] piperan-2 copper-3-(«-cyclopropyl (5- (Fluorenyl-benzyl ester) aminomethyl) furan-2-yl) -4-hydroxy-5, β, 7, 8, 9, 1 0 -hexahydrocyclooctyl [b] piperan-2-one 3- (α-cyclopropyl (5- (N-benzyl ester) aminomethyl) thio -2-ylmethyl) -4 -hydroxy-5, Γ), 7, 8,9, 1 0 -hexahydrocyclooctyl [b] Ninan-2 -copper K-C3- [cyclopropyl (5, 6,7, δ, 9,10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] furanmethyl-2-ylmethyl] 4- Oxybenzene 5 yellow_limb N-[3-[cyclopropyl (5, 7, 7, 8, 9, 1 0-hexahydro-4-hydroxy-2-oxy-2H-cyclooctane [bl piperan-3 -Methyl) methyl] furanmethyl-2-ylmethyl] 4-cyanobenz.tenamine. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling out this page) N- [ 3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4 -hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) yearnyl] thiophene- 2-ylmethyl] 4-cyanobenzene mirrors N-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [h] piperan-3 -yl) methyl] thiophene-2-ylmethyl] 4 -cyanobenzochorpeptide 6 9-This paper size applies to Chinese National Standards (CNS &gt; A4 specifications (210X297 mm) A8 B8 C8 D8 VI. Application scope of patent 3-(«-Cyclopropyl (5-methyl-4-hydroxymethylthiophen-2-ylmethyl) -4-hydroxy-5,6, 7,8,9,10-Hexane [1 &gt;] piperan-2-_ 3-U [S] -ethylbenzyl) -4-hydroxy-5, 6,7, 8, 9, 10-hexahydrocyclooctane [b] piperan-2 -Keto 3- (ct [R] -ethylbenzyl) -4 -hydroxy-5,6,7,8,9, 10-hexahydrocyclooctyl [b] piperan-2-嗣 .Η-[3 -[Cyclopropyl (5,6,7,8,9,10-Hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl ] -N -phenylamine Η '-[3-[cyclopropyl (5, β, 7, S, 9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b ] Piperan-3 -yl) methyl] phenyl] -N, N -dimethylsulfanilamine N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro- 4-hydroxy-2-oxy-2 fluorene-cyclooctyl [M piperan-3 -yl) methyl] phenyl] -4 -methyl-1 -hexahydropyridine_amineN -mosyl-3 -[Cyclopropyl (5, β, 7,8,9,10-hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] -cage Sulfoamine N- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4- mesityl-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -Methyl) Phenyl- (R) -benzenesulfonamide_Printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs (Please read the precautions on the back before filling this page) 4 -Cyano-N-[ 3-[Cyclopropyl (5,6,7, δ, 9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -yl) methyl] Phenyl] -benzenesulfonamide hydrazone-[3-[cyclopropyl (5, β, 7 r8,9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] Amino-3 -yl) methyl] cagel] -4-(dimethylamino) benzyl-4-an- (bromoΦ) [3- [cyclopropyl (5, 6,7,8,9 , 10-Hexahydro-4-hydroxyl_ 2-S Feng-2 Η -cyclooctyl [b] Nanan-3 -yl) methyl] cagel] -Benlu 醯 -70-This paper applies Chinese national standards (CNS> A4 specification (210X297 mm) A8 B8 C8 D8 VI. Application scope of patent 4-[[[3- [cyclopropyl (5, 6, 7, 8,9, 10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -benzylamine N- [3-[cyclopropyl (5,6, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5-(phenylsulfonyl )-, (S) -2-Hyphloline H- [3- [cyclopropyl (5,6,7, 8,9,10 -hexahydro-4-hydroxy-2-oxy-2 Η -Cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -3 -hydroxy-benzylsulfonamide N- [3- [cyclopropyl (5, 6, 7,8,9,10- Hexahydro- 4-Ethyl-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-fluoro-benzenesulfonamide, 4-butoxy-N- [3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] manan-3 -yl) methyl] phenyl] benzene Chloramine 5 -chloro-N- [3-[cyclopropyl (5, 6, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan -3-yl) methyl] phenyl] -1,3-dimethyl-1 Η -pyr beer-4 -sulfonamide. Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before (Fill in this page) 2,4-Dichloro-N-[3-[Cyclopropyl (5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2-oxy-2Η-cyclooctyl [b] Nan-3-yl) methyl] phenyl] benzylamine N- [3- [cyclopropyl (5, (5,7, 8, 9, 10-hexahydro-4-hydroxy-2 -Oxy-2H-cyclooctyl [b] piperan-3-ylmethyl] phenyl] -4-hydroxybenzenesulfonamide 1 9.-A kind of milk used for the infection of human immunodeficiency virus (IVV) The medicinal product that inhibits the retrovirus in animals, among which is a compound of formula I which contains a pharmaceutically acceptable carrier and an effective agent, '-71-This paper is in accordance with China National Standard (CNS) Α4 Grid (210Χ297 mm) patent scope A8 B8 C8 D8 In combination 0 2 R and 0 1 R, a) Or R0 (Read the notes on the back of the poem before filling out this page) (c Π I 8 'R Employees of the Central Standards Bureau of the Ministry of Economic Affairs, Consumer Cooperatives, China, cc, bcd, P', China, China, China, China, etc. 2 papers Standards apply Chinese National Standard (CNS) A4 specifications (210X297 mm) A8 B8 C8 D8 VI. Patent application scope C) -CF3 &gt; d) -0-C η Η 2 η -CH = CH2, or e) -0 -C η. Η ^ η -Η et) or wherein RiR R 2 synthesizes a phenyl group; or wherein R. And RA becomes stupid; where Rs is a) b) -diphenyl. ethyl-: &gt; c) -distyryl--, d) -CH- (C 3 ~ C fi ring healdyl) 2 9 e) -5,6,7, 8, 9-tetrahydro-5H -benzocycloheptenyl f) -1,2,3,4-tetrahydro-naphthyl-0C nH 2 η + 1 * g) -CH (C „Ha η + 1) &quot; C (0)-0-C η Η 2 η + 1 * h) -CH (CH 2-cage) 2 * n -C ^ H a ^ -CH (R 4) -C 『2 V-hetj or ----------- (Please read the notes on the back before filling out this page) Order ^ WK / I Central Standards of the Ministry of Economy 印 Institute of Employee Consumer Cooperatives · j) -CwH-av-CH (R4 .)-CvHav-het-R5; where 1 is b)-CH a-C (0)-0-C „H ^ n. A &gt; c) -C3-C« cycloalkyl, or d)-C „H 2-C 3-C e ring comprehensive foundation; -73-This paper size applies to China National Standard (CNS) A4 (210X297 mm) Printed by A8 B8 C8 D8 of the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs The scope of patent application where R 5 is a) -Η, b) -HHa &gt; 〇) _C ⑻- CnH2 ..., d) (ortho) or (meta) -〇-CnH2n'CH = CH2, e)- Ci-U alkoxy * is 0 or 1 at each carbon atom F) -0-C (0) -CnH ^ n ,! &gt; g)-B r »h) -CN, i) -CmHani-Xl-C-RH2t + T '.3) &quot; Xi-CnHan-® &gt; 'k) KUH «, Π -Xi-CnH2n-NH-C (0) -0-CnH2„ .am) -Xi-CnHZn-CH (HH-C (0) -0- C „H2t, * n.) C (0) -0- η H 2 n-&gt;-T * n) -X'-T'mHam-OH (NH-C (0)-O- CnHiJn + l) -CnHan- H et, »O) -X ^ -CnHiin-CH (NH2) CGOH« P) -Xl-C ,, H2r, -C (0) -〇-CnH2n-T »q)-X '-c „H 2„-C 3-C e cycloalkyl, Γ)-"'mHzm-Xl-CmHaTn -aryl,-s) -Xi-CmHzm-Π-aryl, t,) -Xl-CmH2m-〇 -CnH2r, + i &gt; -74-This paper size is applicable to Chinese National Standard (CNS) A4 (210X297 mm) (Please read the precautions on the back before filling this page) Printed by the Consumers' Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A8 B8 C8 D8 VI. Patent Application Range U) -CmHzm-Xl.-CmH2m-Het &gt; V)-XX-C Π Η 2 η-C (0)-H et »w) -Xi-CnHan-C (0) -NH-CnHar, -Het &gt; X) -Xl-CnHar.-S-Het» y) _CmH2m-X, .-〇-CnH2n_ aryl, z) -CmH2ra-Xl-〇-CnH2n-Het »al) -X ^ -H &gt; b1) -Xx -CH = CH2« cl) -Xi-CH = CH-aryl, d 1)-X t-H ( R 4 〇) 2. El) -Xa-CnHh-P: bacterimine, fl) -Xα- (pentafluoro) -phenyl * gl) -Xi-C „H2„ -Bicyclic [2 · 2 · 1 ] Heptane, hi) -C, j-H2U-R3〇 * Π--N = C-(NH-CH (C „H an. X) a) 2. Jn -N HP (0) (RQ)- Aryl, kl) -NH-iMOHO-Rn) -aryl, m-NH-C (S) -NH-R42, or ml) -NH-C (S) -CHa-Rd;?; Where Xx is a )-N HC (0)-&gt; b)-C f 0)-NH-»c) -NH-S02-, d) -S02-KH- * -75-This paper is compatible with Chinese National Standard (CNS) A4 specifications (210X297 mm) 41. (Please read the precautions on the back before filling out this page) Order A8 B8 C8 D8 VI. Patent application scope e) -HH-SOz-HH- * f)-C (0 )-Q-. G)-0-C (0)-&gt; h) -N (C „H2„ -aryl)-(:( 0)-, i) -NH-C (0) -NH- , Or j) -N [(CnH2 „) aryl] -S02-; where m is from 0 to 5; where n is from 1 to 5; where P is from 1 to 8; where q is from 0 to 5; Where r is from 1 to 8; where s is from 1 to 6 ·, where t is from 1 to 1 2; where υ is from 2 to β; where ν is from 0 to 2; where aryl is a) phenyl Is replaced by 0 to 3 1U, b) naphthyl is replaced by 0 to 3 R «, or c) bibenyl is replaced by 0 to 3 1U; printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please Please read the notes on the back before filling out this page) where Het. Is a 5- or (5-membered saturated or unsaturated ring, containing 1 to 3 heteroatoms selected from the following, including: nitrogen, oxygen and Tellurium, and includes any bicyclic group, wherein any one of the above heterocyclic rings may be fused with a dull ring or another heterocyclic ring; and the ring may be connected via a carbon or a second nitrogen on the ring or an exocyclic nitrogen; and if chemical It is suitable for the above purpose.! 丨 Nitrogen and thorium atoms can be in an oxidized form; and if -76-This paper size applies to Chinese National Standard (CNS) A4g ( 210X297 mm) 々, the scope of the patent application is chemically suitable, the nitrogen atom may be in a protected form; and it is substituted by 0 to 3 RVs; wherein R β and R 7 are independent a) -Ci-C5 alkyl groups, Substituted with 0 to 3 halogens, or 0 or 1 hydroxyl at each carbon atom, b) -OH, c)-(^-(: 5alkyl-(^, d) -d-Ci -Cs alkyl is substituted by 0 to 3 halogens, or 0 or 1 hydroxyl on each carbon atom, (Please read the precautions on the back before filling this page) E) -0-C2-C7 dilute group, which is substituted by 0 or 1 hydroxyl group, f) halogen, g) -nh2, h) -N Η 2-C τ-C 5 complex, i) single or two -Cl -C5 alkylamino, j) -NH-OH &gt; k) -N (CH 2-0 H) 2 &gt; 1) -C (0)-NH a &gt; m) -f: (0) -C τ-C 5 heald, n) -CH0 &gt; o) -C00H &gt; p) -cox2, q) nitro, Γ) -CN &gt; s) -s〇3h &gt; -77-This paper Standards are in accordance with Chinese National Standards (CNS) A4 «&lt; Grid (210X297 mm) Patent Application Scope t.) U) V) Vi) x) A8 B8 C8 D8 -S02HH3 &gt; -S02-phenyl is substituted by 0 to 3 R12, -N Η-S Ο 2 -phenyl is substituted by 0 to 3 R 2, -SOa-HH- Phenyl is substituted by 0 to 3 R12, -0 [(CH2) 20] qCH3, Y)-C ⑻-Ο-C „Η… α, ζ)-Ν Η-C (Ο)-C η Η ^ α. nl) -C „H2n-NH-C (0) -phenyl, b 1)-Ν = Ν -phenyl, 0 or 1 -N (C„ Η 2 „c 1.) Oxazolyl, ril) pyridinyl,) a substituted el) -Xs-Uau-R f 1) morphyl; g 1) hexahydropyridyl, h) hexahydropyridyl, Π)-HR 4 〇R ^ t ».i 1)-Π R 4 〇 '3 Ο ------- ^ --------- Order (Please read the notes on the back before filling this page) kl ) • NH- -SO, X or printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (CH2) u 1 1)-C η H i &gt; η ~ 0-C η Η 2 η-0 C η Η -Where X 3 is 3)-0-, η Π 2 η * ♦ · Τ The paper size is applicable to the Chinese National Standard (CNS) A4 specification (210 × 297 mm) 6. Scope of patent application b) -CHa-Q- »C ) -sn〇-, d) ~ NR4.〇S〇2- &gt; e) -c (0)-, f) -C (0) hr4〇-- g) -HR4〇C (0), or h) ~ NR 4〇- &gt; A8 B8 C8 D8 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs where R f »is a) -Η, b)-C 2 „-fluorenyl is substituted by 0 to 3 R β, C)-C r, 2 η-H e t. &Gt; d)-C n H 2„-C 3- C cycloalkyl, ft) -C ^ -Hzr '+ l, f) -c.h2 „-ch = chz &gt; g)-C β 2 3 +,. Is substituted by 1 or 2 hydroxyl groups, h) -C Η 2 -epoxide, π -γ ^ η2 „-Ethylene oxide, • j)-(Cr, H2n-〇) n_CnH2n * l * k)-C (〇)-C β Η 2 sq , Or l)-C. Η (Ο Η)-C 3-C β cycloalkyl; where! "Is a) -Ci-U fluorenyl, or b) aryl; where R 1 1 is (Please read the notes on the back before filling in this f) Peak -79-This paper size applies Chinese National Standard (CNS) A4 specification (210 X 297 mm) A8 B8 C8 D8 Patent application scope Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs a) -H, b) -Ci-C4 alkyl, c) aryl, or d) its pharmacy In the above connection, R α 2 is a) Cx-C3 alkyl group, b) Cl_-C3 comprehensive oxygen group * c) dimethylamino group, d) diethylamino group, e) CF3, f) Π N &gt; g ) Halogen, h) -NH2, i) -OH &gt; -j) -C (0)-, or k) -sm; wherein R 3 Ο is b) hexahydropyridyl, c) hexahydropyridyl, d) -NR4.0R4-T * e) Ho, f) —NH-SO- \ / '(CH ^ 3) Mo Fu Zhi Ji 8 0-(Please read the notes on the back before filling this page) This paper uses Chinese National Standard (CNS) A4 specifications (210X297 cm). 6. Scope of patent application. G) Methyl-hexahydropyridine. H) Halogen; And R Λ 1 independently select a) -H or b) ~ C 1 -C 4 alkyl; wherein R 4 2 is a) C tC 4 alkyl, or b) phenyl; the restriction is ... 1) When m— is independent -H or -〇CH3, R3 is part of formula IV and + &gt; SJi R 6-Η-Ο C Η 3; 2) when R 5 is -C VH 2-X α- Ο-U Η 2 -aryl or -CmH2m-Xi. -Q-CnHzn-Hfit, Xι is not-〇 (Π) _ΝΗ-., -Η Η S 〇 ^-, -SOa-HH- &gt; -Ν Η -S Ο a-Ν Η---C (Ό) -〇- &gt; -OC (O)-, -rrt-C (0) -NH-, -MUUU-aryl] -S02-; and Ministry of Economic Affairs The Central Bureau of Standards and Consumers ’Cooperatives (Please read the precautions on the back before filling out this page) 3) When R 4 is -Η in the formula iV part, then R 5 is a substituent containing X i, of which) U is -NHSD2-; and its pharmaceutically acceptable salts. 20 · The peony drug product according to item 19 of the scope of patent application, wherein the compound is selected from the group consisting of the following: 3- (cyclopropylfluorenylmethyl) -5,6,7,8,丨), 10-hexahydro-4-hydroxy- -81-This paper is compatible with Chinese National Standard (CNS) A4 (210X297 mm) 6. Application scope of patent 10- (2-hydroxy-1-methylethyl ) -2H-cyclooctyl [b] piperan-2- 嗣 3- (cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-10- (: 2-hydroxypropyl) -2 ^ cyclooctane [1 &gt;] piran-2-copper 3- (cyclopropylphenylmethyl) -5, Γ), 7,8,9,10-hexahydro-4 -Hydroxy-10- (oxiranylmethyl) -2'-cyclooctyl [b] piperan-2-one. 3-[(3-Aminophenyl) cyclopropylmethyl] -5,6,7,8,9,: 10-hexahydro-4-hydroxy-2H-cyclooctan [b] nanan-2-one Aminocarboxylic acid, [3-[[3- [Cyclopropyl (4-hydroxy-2-oxy-2H-bubenzopiperan-3-yl) methyl] .phenyl] amino] -3- Copper propyl]-, 1, dimethyldimethylethylaminocarbamate, [3- [cyclopropyl (4-hydroxy-7-methoxy-2-oxy-2 fluorene)-:!-Benzo Piperan-3 -yl) methyl] benzyl]-, phenylmethyl ester carbamic acid, [3-[[3- [cyclopropyl (4-hydroxy-7-methoxy-2-oxy -2Η-1-benzopiperan-3-yl) methyl] phenyl] amino] -3-fluorenyl] 1,1-dimethylethyl coumarin, 4-hydroxy-3- (α-(3-(. (3-1 Η-indole-1 -yl) -1-嗣 propyl) amino) phenyl) cyclopropylmethyl) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (#Please read the notes on the back before filling this page) Coumarin, 4-hydroxy-3- (1-benzylpropyl) -7-propoxy, 3- (cyclopropylphenylmethyl)- 5, β, 7,8,9,] 0-hexahydro-4-hydroxy-l0-[(tetrahydro-2-furanyl) methyl] -2H-cyclooctyl [b] piperan-2-copper 3 -(Cyclopropylphenylmethyl) -5,6,7,8, 9, 10 -hexahydro-4-hydroxy-10 -[(Tetrazol-2-furanyl) methyl] -2H-cyclooctyl [h] piperan-2-fluorene 3- (cyclopropylphenylmethyl) -5, β, 7,8,9, 10 -Hexahydro-4-hydroxy-10- [2- (2-methoxyethoxy) ethyl] -2Η-cyclooctane. [B] 那 然 _-2-铜 -82-This paper is for China National Standard (CNS) A4 Specification (210X297 mm) A8 B8 C8 D8 VI. Application for Patent Range 3- (Cyclopropylbenzylmethyl.yl) -5,6,7,8,9,10-hexahydro-4 -Hydroxy-10- (hydroxymethyl) -2H-cyclooctyl [b] piperan-2-one 3- (cyclopropylbenzylmethyl) -5,6,7,8, 9, 10 -hexahydro -4-hydroxy-1 0-(1 -fluorenyl) -2 fluorene-cyclooctyl [b] piperan-2-one-3 (cyclopropylphenylmethyl) -5,6,7,8, 9,10-hexahydro-4-hydroxy-10-U-hydroxy-1-methylethyl) -2H-cyclooctane [b] piperan-2-copper 10- (cyclopropylhydroxymethyl)- 3- (cyclopropylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-211-cyclooctyl [1]] piran-2-_ 3- (cyclopropyl Phenylphenylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-1 1-(methoxymethyl) -2 Η -cyclooctyl [h] piperan-2-嗣 3- (Cyclopropylcylmethyl) -5,6,7,8,9,10-hexahydro-4-hydroxy-1O- (2-methoxyethyl) -2H-cyclooctyl [ b)? nan-2- 嗣 3- (ring Phenylphenylmethyl) -5,6,7,8,9,10-hexaargon-4-hydroxy-10-[(tetrahydro-2H-piperan-3-yl) methyl] -2H-cyclooctyl [b] piperan-2-one • 3- (cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9- [2- (2-methoxyethoxy ) Ethyl] cycloheptyl [b] piperan-2 (5 Η)-_ 3- (cyclopropylphenylmethyl) -β, 7,8,9-tetrahydro-4-hydroxy- ζΙ-β -ί 2-(2 -methoxyethoxy) ethoxy] ethyl] -cyclohepta [b] piran-2 (5 Η)-嗣 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please first Read the notes on the back and fill in this page) 3- (Cyclopropylphenylmethyl) -β, 7,8, 9 -tetrahydro-4-hydroxy-9- (phenylmethyl) -cycloheptane [b 1 piperan-2 (5Η) -one 3- (cyclopropylphenylmethylW), 7, 8, 9-tetrahydro-4-hydroxy-9- (2-methylpropyl) -cycloheptane [b] Piran-2 (5H) -one 3- (cyclopropylcylmethyl) -β, 7,8,9-tetrahydro-4-hydroxy-9- (3-methyl-83-this paper Standards are applicable to Chinese National Standard (CNS) A4 specifications (210X297 mm). 6. Patent application scope. Butyl) cyclohepta [b] piperan-2 (5H)-(3- (cyclopropylbenzylmethyl)- 9-ethyl-6,7,8,9-tetraoxy-4- -Cycloheptyl [b] piperan-2 (5 Η)-詷 3- (cyclopropylphenylmethyl) -9- [2- (1,3-dioxocane-2-yl) ethyl ] -β, 7,8,9-tetrahydro-4 -hydroxy-ring, [b] piperan-2 (5 Η) -one 3-(cyclopropylphenylmethyl) -6,7,8, 9-tetrahydro-4-hydroxy-9-[(tetrahydro-2H-piperan-3-yl) methyl] -cycloheptane [b] piperan-2 (5H) -copper 3- (cyclopropylbenzene Methyl) -β, 7,8,9-tetrahydro-4-hydroxy-9-propyl-cyclohepta [b 1piperan-2 (5 Η) -one 3- (cyclopropylphenylmethyl) ) -6,7, 8, 9-tetrahydro-4-hydroxy-9-[(tetraki-2-sulfanyl) methyl.yl] -cycloheptan [b] nanan-2 (5H) -one 3- (Cyclopropylphenylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-9-[(tetrahydro-2H-piperan-2-yl) methyl] -cycloheptane [h] Piperan-2 (5H) _one 3- (cyclopropylphenylmethyl) -β, 7, δ, 9-tetrahydro-4-hydroxy-9-[(tetrahydro-3 -furyl) methyl ] Cyclohepta [b] Nanan-2 (5 Η)-嗣, 3- (cyclopropylS-methyl) -β, 7,8,9-tetrahydro-4-hydroxy-9- (2-hydroxypropane Yl) cycloheptyl [b] piperan-2 (5 Η) -one 3-(cyclopropylcylmethyl) -β, 7,8,9-tetrahydro-4-hydroxy-9- (methoxyethyl Base) -Cyclopepta [b] Piran-2 (5 Η) -Employee of Central Bureau of Standards, Ministry of Copper Economy Fei Cooperative Co., Ltd. (Please read the precautions on the reverse side before filling out this page) Methoxyethyl) cycloheptan [hipiperan-2 (5H) -one 9-(cyclopropylhydroxymethyl) -3- (cyclopropylbenzylmethyl) -β, 7,8,9- Tetrahydro-4 -hydroxy-cyclohepta [b] piperan-2 (5 Η) -anthanoic acid, [3-[[3- [cyclopropyl (5, 6, 7, δ, 9, 10- Hexahydro-4- -8 4-This paper size applies to China National Standard (CNS) A4 (210 × 297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A8 B8 C8 D8 Oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino.]-3 -copperpropyl]-, 1,1-dimethylethyl ester 1H-indole -Propane amine, H- [3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] benzyl] -aminocarboxylic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] limyl] -Bu (S) -methyl-2-ketoethyl]-, 1,1-dimethylethyl Ester urethane, [2-[[. 3- [ Propyl (5,6,7,8,9,10-hexahydro-4_hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl.] Benzyl] amino ] -1-[[1- (S)-[(4-Tolyl) sulfonyl] -1H-imidazol-5-yl] methyl 1-2 -ethyl]-, 1,1-dimethyl Ethyl ester aminocarboxylic acid, [2-[[3- [cyclopropyl (5, 6,7,8, 9,10-hexahydro- 4-hydroxy-2 -oxy-2 Η -cyclooctyl [b ] Piperan-3 -yl) methyl] phenyl] amino] -2-oxoethyl]-, 1,1-dimethylethyl ester aminocarboxylic acid, [4-[[3- [cyclopropyl (5, 6,7,8, 9, 10 -hexahydro- 4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] amino] -4 -oxobutyl]-, 1,:!-Dimethylethyl ester 1 (S) -pyrrolidinecarboxylic acid, 2-[[[3- [cyclopropyl (5, ί5,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] carbonyl]-, 1,1-dimethyl Ethyl ester aminocarboxylic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 氧基 -cyclooctyl [h ] Piran-3 -yl) methyl] phenyl] amino] -B (R) -methyl-2 -oxoethyl]-, 1, 1 -dimethylethyl ester -85-paper size Apply Chinese National Standard (CNS) A4j ^ lattice ( 210X297 mm) (Please read the notes on the back before filling this page) 6. Scope of patent application • Anthracenecarboxylic acid, [2-[[3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro- 4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -imidazol-4-ylmethyl) -2-methylethyl]-, 1,1-dimethylethyl ester 1-hexa Hydroxamidine propylamidine, N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan -3-yl) methyl] phenyl] benzamidine, 4-chloro [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclo Octyl [b] piperan-3-yl) methyl] phenyl] -N- [3- [cyclopropyl (5, t5,7,8,9,10-hexahydro-4-hydroxy-2-oxy -2 fluorene-cyclooctyl [b] piperan-3yl) methyl] phenyl] -benzylethylamine N-[3-[cyclopropyl (5, 6, 7, 8, Q, 10-6 Hydrogen-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -3 -phenyl-2 -propylene fluorene N- [3-[cyclo Propyl (5,6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -butane Printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Brewery and Economics (please read the notes on the back before filling this page) 鞍 _ Saddle, N-[3-[cyclopropylί 5, Γ) 7,0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -4 -fluoro- (cetomine, N- [ 3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 羟基 -cyclooctyl [b] piperan-3-yl) methyl] benzene Yl] naphthylcarboxamide, N- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2Η-cyclooctyl [b] piperazine Alan-3-yl) methyl] phenyl] -carboxylic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4_hydroxy-2-oxo -2H-cyclooctyl [h] piperan-3-yl) methyl] phenyl] amino] ~ 8 fi-This paper size applies to China National Standard (CNS) A4 (210X297 mm) ABCD VI. Application Scope of patent-imidazol-4-ylmethyl) -2 -fluorenylethyl]-, 1,4-dimethylethyl ester aminocarboxylic acid, [3-[[3- [cyclopropyl (2,5,6 , 7,8,9-hexahydro-4-hydroxy-2-cycloheptyl [b] pulsan-3-yl) methyl] phenyl] amino] -3-fluorenyl]-, 1,1- Dimethyl ethyl ester dH-indole-1-propanamine, N- [3- [cyclopropyl (2,5,6,7,8,9-hexahydro-4 -hydroxy-2 -'one Cycloheptane '[b] piperan-3 -yl) methyl] phenyl] -carbamic acid, [2-[[3- [cyclopropyl (5,6,7,8,9,10-hexahydro -4-hydroxy-2 -oxy-2 H- Cyclooctyl [b] piperan-3-yl) methyl] phenyl] (phenylmethyl) fluorenyl] -2-oxoethyl]-, 1, dimethyldimethylethylaminocarbamate, [ 3- [1- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl l_b] manan-3 -yl) propyl] phenyl]-, Phenylmethyl alcohol 2 Η -cyclooctyl [b] piperan-2-_, 3-[1-(3-aminophenyl) propyl] -5, 6,7,8,9,10-hexahydro 4-hydroxy-aminocarboxylic acid, [3-[[3-[1-(5, 6, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2-oxy-2 2H-cyclooctyl [ b] piperan-3-yl) propyl] phenyl] limyl] -3-ketopropyl]-, 1,1-dimethylethyl ester Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economy — (please first Read the notes on the back and fill in this page) Propylamine, 3-amino-N-[3-[1-(5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2- Oxy-2Η-cyclooctyl [b] piperan-3-yl) propyl]. Phenyl]-, monohydrochloride mesotriamine, 4 -aero- •?)-[3- [1- (5,6,7. 8,9,10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [h] piperan-3 -yl) propyl] phenyl]-ceramide_, 4-fluorenyl- N- [3- [l- (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) propyl] Phenyl]--87-This paper size is applicable to China National Standard (CNS) A4 specification (210X297gm) A8 B8 C8 D8 6. Application for patents , 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N'-ethylureamidine- [3- [ Cyclopropyl (5,6, 7,8,9, 10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N '-Phenyl gland [3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl ) Methyl] phenyl]-, benzyl ester aminocarboxylic acid [3-[cyclopropyl (5, β, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2 -2--Η- Cyclooctyl [b] piperan-3-yl) methyl] phenyl]-, ethyl ester carbamic acid 2 Η-cyclooctyl [b] piran-2-copper, 5, 6, 7, 8, 9 , 1 0 -hexahydro-4 -hydroxy-3- (2-methyl-buphenylpropyl)-i +)-U) -3- (cyclopropylphenylmethyl) -5, β, 7 , 8,9,10 -hexahydro-4 -hydroxyl -2 Η -cyclo [b] piperan-2-瘌 (:-)-(S)-3-(cyclopropylphenylmethyl) -5,6,7,8,9, 1 0 -hexahydro -4 -hydroxy-2 -2 -cyclo [b] piperan-2 -copper (R or S)-3-(cyclopropylbenzylmethyl) -fi, 7,8,9 -tetrahydro-4 -hydroxy -Cycloheptan [b] piperan-2 (5 Η)-_ or S) -3- (cyclopropylcylmethyl) -6,7,8,9-tetrahydro-4-hydroxy-cycloheptane [ b] Piran-2 (5 Η)-嗣 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 3- (R)-(cyclopropylphenylmethyl) -4 -hydroxy-10- (R and S) -propyl-5, 6. 7,8,9, 10 -Hexahydro-cyclooctyl [b] piperan-2- 嗣 (cyclopropylphenylmethyl) -4-hydroxy-10- (R or S) -propyl-5.  6 f 7 J, 9, 1 0 -Hexahydro · -cyclooctyl [h] piperan-2-嗣 3-(R)-(cyclopropylphenylmethyl) -4 -hydroxy-1 0-(R Or S) -propyl-5,6,7,% 9, 10-hexahydro-cyclooctane [b] piperan-2-one-8 8-This paper uses Chinese National Standard (CNS) A4 specifications ( 210X297 mm) A8 B8 C8 D8 VI. Application scope of patent 3- (S)-(cyclopropylbenzylmethyl) -4-hydroxy-10- (R and S) -propyl-5, 6, 7, 8, 9, 10-Hexahydro-cyclooctyl [b] Nanan-2-copper 3- (S)-(cyclopropylphenylmethyl) -4-hydroxy-10- (R or S) -propyl- 5,6, 7, 8,9, 10-hexahydro-cyclooctyl [b] piperan-2-one / 3- (S)-(cyclopropylbenzylmethyl) -4 -hydroxy-10- ( R or S) -propyl-5. 6,7,8,9,] 0-hexahydro-cyclooctyl [b] piperan-2- 喃 · fluorenylcarboxylic acid, [2-[[3- (R or S)-[cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] -2 -fluorene Group]-, 1, dimethyl ethyl ester aminocarboxylic acid, [2-[[3- (R or S)-[cyclopropyl (5,6,7, δ, 9,10) _hexaki 4-Hydroxy-2-oxy-2H-cyclooctyl. [b] Where: ran-3-yl) methyl] penyl] amino] -2-ketoethyl]-, 1, dimethyldimethylethylaminocarbamic acid, [2-[[3- ( R or S)-[cyclopropyl (5, 6, 7,8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl ] Phenyl] amino] -l- (S) -nH-imidazol-4-ylmethyl) -2-. Copper ethyl]-, 1,1-dimethyl ethyl ester (Please read the notes on the back before filling out this page) Acid methyl T amine. Hydrogen hexa or radical.  Oxygen J 2 I based hydroxycyclopropane. Piperidine bl Printed with octylcyclomethanine at the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. -Ylbenzene [bmethyl1 octylamino1 benzene 1 'I-_yl W methyl]} ylethyl 3-ketoformyl I. 2 I n-piperazinyl-cyclopropylmethyl _-.  Phenylbenzene J-1 amine \-ylethyl benzyl hydroxy-4 I nitrogen hexafluoro I 2 I  Pipeline _-rb ί __- The size of this paper is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 6. Scope of patent application [3- [cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N- (benzyl) -benzenesulfonamide hydrazone- [3 -[Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2-2--cyclooctyl [b] piperan-3-yl) methyl] phenyl] -Fluorene- (phenylmethyl) -methanesulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10 -hexahydro-4-hydroxy-2-oxy-2H- Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N- (2-phenylethyl) -benzenesulfonium_amine '· (-)-3-[(3-aminophenyl) Cyclopropylmethyl] -5, β, 7,8,9,10-hexahydro-4 -hydroxy-2-4-cyclooctyl [b] piperan-2-one; and (+)-3-[( 3-aminophenyl) cyclopropylmethyl] -5, (5,7,8,9,10-hexahydro-4-hydroxy-2 «-cyclooctyl [b] piperan-2-one-(- ) -3- [Cyclopropyl- [3-limyl] phenyl] methyl] -5,6,7,8,9, 10 -Hexahydro-4 -hydroxy-2 -2-cyclooctyl [b] Nan-2-_ (+)-3- [cyclopropyl- [3-amino] -5, (5,7,8,9,1 0 -hexahydro-4 -hydroxy-2H-cyclooctyl [b ] Piran-2- 嗣 Staff Consumers, Central Bureau of Standards, Ministry of Economic Affairs Printed by the cooperative (please read the precautions on the back before filling this page) (-)-4-氡-N- [3- [cyclopropyl (5,6,7,8,9,10 -hexahydro-4 -Hydroxy-2-oxy- 2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonamide (+)-4-ammonium-H- [3-[cyclopropyl (5,6,7,8, 9, 10-hexahydro-4-hydroxy-2 -oxy-2H-cyclooctyl [b] mannan-3-yl) methyl] benzyl] -benzyl vine limb ( -)-N-[3-[cyclopropyl (5, Γ), 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy- 2H -cyclooctane [b] piperan-3 -Yl) methyl] benzyl] -4 -fluoro-benzene. Lumenamine (+)-N-[3-[cyclopropyl (5, 6, 7, 8 f 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-90-This paper size applies to Chinese national standards (CNS) A4 specification (2! 0X297 mm) A8 B8 C8 D8 VI. Patent application scope Base-2Η-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -4-fluoro-benzene Amine (-) 1- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooct-3-yl) methyl] Phenyl] -1-methyl-1H-imidazole-4-sulfonamido (-)-4-cyano-K- [3- [cyclopropyl (5, β, 7, 8, 9, 10 -hexa Hydrogen-4-hydroxy-2-oxy-2Η-cyclooctyl [b] anan-3-yl) methyl] phenyl] benzene code rattan (-)-(^-[cyclo [( 5,6,7,8,9,10-hexaaza-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -8-BS Amidine • (-)-H- [3- [Cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 hydrazone-cyclooctyl [b] piperazine Uran-3-yl) methyl] phenyl] -2-phenyl-[(E)]-vinylamine [cyclopropyl (5,6,7,8,9,10-hexahydro-4- Hydroxy-2-oxy-2H-cyclooctyl [b] nanan-3-yl) methyl] benzyl] -benzylcarboxyl-4 -cyano-N-[3-[cyclopropyl (5, 6 , 7, 8, 9, 10 -Hexahydro-4 -hydroxyl -2-Oxygen-2H-cyclooctyl [b] anan-3-yl) methyl] phenyl] -benzylamine (+)-N-[3-[cyclopropyl (5, β, 7, 8,9, 1 0 -Hexahydro-4 -hydroxy-2 -oxy_2Η_cyclooctyl [b] mannan_3_yl) methyl] phenyl] -8 -Luo lanase amine Central Ministry of Economic Affairs Standard Printed by the Bureau's Consumer Cooperative (please read the precautions on the back before filling this page) (+-[3- [cyclopropyl (5,6,7,8,9,10 -hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl · phenyl] phenyl] -2-¾yl-[(E)]-ethylenesulfonylamine 4 -cyano-N- [ 3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [h] piperan-3-yl) methyl] cyl ] -Bensulfonamide ~ 91 This paper size is applicable to China National Standards (CNS) A4 ^ (21 ×: 297 mm) Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs A8 B8 C8 D8 6. Scope of patent application N- [3- [cyclopropyl (5,6, 7, 8, Q, 10-hexahydro-4-hydroxy-2-oxy-2 K-cyclooctyl [b] piperan-3 -yl) formyl Yl] benzyl] -8-D-quinolinesulfonamide 4-chloro-fluorene- [3- -cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-oxy- 2Η-cyclooctyl [b] mannan-3-yl) methyl] phenyl ] -Benzenesulfonamide N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan- 3-yl) methyl] phenyl] -4- (1,1-dimethylethyl) -benzenesulfonamide N- [3- [cyclopropyl (5, β, 7, 8,9,10 -Hexahydro-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] cagel] -2 -naphthosulfonamide hydrazone- [3- [cyclopropyl (5, 卩), 7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2-4--cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- ( Trifluoromethyl) -benzylamine [3- [cyclopropyl (5,6,7,8, 9, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Manan-3-yl) methyl. ] Phenyl] -4-Gas-benzylamine &gt; 3-4-Difluorene-N- [3- [cyclopropyl (5, β, 7, S, 9,10-hexahydro-4-hydroxyl -2 -oxy-2 hydrazone-cyclooctyl [b 1piperan-3 -yl) methyl] phenyl] -benzenesulfonamide hydrazone-[3-[cyclopropyl (5, β, 7,8, 9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -1 -naphthalenesulfonamide 2, 5-di Chloro-N- [3- [cyclopropyl (5, 6,7, 8, 9, 10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [h] piperan-3 -yl ) Methyl] phenyl] -benzylsulfonylamine 4-methyl- [3-[cyclopropyl (5, β, 7,8,9,1 0 -hexahydro-4 -hydroxy-2 -oxy- 2Η-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzimidamine H- [3- [cyclopropyl (5, Γ), 7, 8, 9, 10-hexahydro -4-Hydroxy-2-oxy-2 fluorene-cyclooctyl [h] piperan-3-yl) methyl] cagel] -4 -nitro-sulfonylsulfonium 9 2 This paper is applicable to Chinese national standards (CNS) 8-4 specifications (210X297 mm) (Please read the notes on the back before filling in this I) 丨 «Axes 丨 Sixth, the scope of patent application * N- [3- [cyclopropyl (5, β, 7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] benzene ] -3-nitro-benzylsulfonamide N- [3- [cyclopropyl (5, β, 7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [ b] lanan-3-yl) methyl] phenylbut 4-methoxy-benzenesulfonyl 4-[[[3- [cyclopropyl (5, Γ), 7,8, 9, 10- Hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfonyl] -benzoic acid N- [3- [cyclo Propyl (5, 6,7,8, 9, 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -2 , 4, β-trimethyl-benzylamine hydrazone-[3-[cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2 -oxy-2 hydrazone- Cyclooctyl [b] piperan-3 -yl) methyl] benzyl] -2,3,4, Γ), 6 -pentafluoro- • cagesulfonate-[3-[cyclopropyl (5, R, 7,8,9,1 0-Hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b 1piperazin-3 -yl) methyl] phenylbuthyl 2,4-dioxo -Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economics of Besulfene (please read the precautions on the back before filling this page) N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10 -Hexahydro-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] cyl] -3-(trifluoromethyl) -benzyl N-[3-[cyclopropyl (5,6,7,8,9,1 0-hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [Mpiperan-3-yl) methyl ] Phenyl] -2-fluoro-benzenesulfonamide 4-butoxy-N- [3- [cyclopropyl (5, β, 7, S, 9,10 -hexahydro-4-hydroxy-2- Oxygen =%-2Η-Cyclooctyl [b] ?: Nan-3-yl) methyl] benzyl] -benzylamine-9 3-This paper size applies to China National Standard (CNS) A4 (210X297 mm) ） 6. Scope of patent application • K- [3- [cyclopropyl (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2 Η-cyclooctyl [b] piperazine Ran-3yl) methyl] phenyl] -5-(dimethylamino)-: L-naphthalenesulfonylamine 3,5-dichloro-N- [3- [cyclopropyl (5,6,7 , 8,9, 10-hexahydro-4-hydroxy-2 -oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -2 -carboxybenzylidene 2, 3-Difluorene-Bu [3- [cyclopropyl (5, "), 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl Lb] anan-3- Methyl) benzyl] -benzyl-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 H-2 Cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-\ trifluoromethyl) -benzene 5 «i§ P 2 -Ga-hydrazone-[3-[cyclopropyl (5, f), 7, 8, 9, 10-hexahydro-4 -hydroxyl -2 -oxo-2Η-cyclooctyl [b] manan-3-yl) methyl] phenyl] -β-methyl-benzene basis He Jun.   3,5-Difluoro-N- [3-[cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2 -oxy- 2Η-cyclooctyl [h] pyran -3-yl) methyl] phenyl] -benzene basis _ Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page). 3-氡 -Η-[3-[cyclopropyl (5, β, 7, δ, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b] piperan- 3 -yl) methyl] phenyl] -sulfenylsulfonium N- [3- [cyclopropyl (5,6, 7, 8. 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] Nanan_3 · _ volume) methyl] phenyl. 丨 -4 · -Benzyl chloride 3-bromo 1- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy- 2Η-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -benzenesulfenamine 3-[[[3- [cyclopropyl (5,6,7. 8, 9, 10-hexahydro-4-hydroxy. -2-oxy-2 hydrazone-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfonyl] -benzyl-94-This paper uses the Chinese National Standard (CNS ) A4 ^ (210X297 mm) ABCD VI. Application scope of patents, 2-chloro-N- [3- [cyclopropyl (5, Γ), 7,8,9,10 -hexahydro-4-hydroxy- 2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -benzenesulfonamide 5-ammonia-N- [3- [cyclopropyl (5, (5, 7, 8,9,10-hexahydro-4-meryl-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -1,3-dimethyl- &quot; I Η -Shame-4 _ ξ®. Tamine, 2, Γ) -dichloro-fluorene-[3-[cyclopropyl (5,6, 7, δ, Q, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 2 -cyclooctyl [ b] piperan-3-yl) methyl] benzyl] -bensulfonamide * N- [[5-[[[3- [cyclopropyl (5,6,7,8,9,10-hexa Hydrogen-4-hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] sulfofluorenyl] -2-thienyl 1methyl Amine hydrazone-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctane-3 -yl) methyl] phenyl ] -1 -Methyl- (S)-1 hydrazone-oxazole-4 -sulfo-amine N- [3- [cyclopropyl (5, 6,7U, 10-hexahydro-4-hydroxy-2-oxyl -2 hydrazone-cyclooctyl [b] piperan-3-yl) methyl] benzyl 1-4-(benzene-sulfosulfanilamide) -2 -exposed phenoloxine, Consumers Cooperative of Central Standards Bureau, Ministry of Economic Affairs Printed (Please read the precautions on the back before filling this page) N-[3-[Cyclopropyl (5, Γ), 7, 8, 9, 1 0 -Hexahydro, 4 -Hydroxy-2 -oxyl -2 hydrazone-cyclooctyl [b] piperidin-3-yl) methyl] phenyl] -5-(phenylsulfonamido) -2-methylphenamine amine N- [3- [cyclopropyl ( 5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4-iodo- Sulfonamide 5 -Chloro-N-[3-[Cyclopropylammonium (5 JK7,8, 9, 10 -Hexahydro-4-hydroxy- 2-oxy-2 hydrazone -cyclooctyl [b] piperan-3 -Base) methyl-based] $-based] -2 -thiophenesulfonamide-9 5-This paper uses Chinese National Standard (CNS) A4 specifications (210X297 mm) A8 B8 C8 D8 6. Application for patent scope 4, 5 -dichloro-N- [3- [cyclopropyl (5,6, 7, 8,9,10 -hexahydro-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan- 3 -yl) methyl] phenyl] -2-thiophenesulfonamine-4,5-dibromo-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4 -Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-thiophenesulfonyl 2/5 -dichloro-N- [3- [cyclopropane (5, 6, 7,8, 9, 10-hexahydro-4-hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -3- Thiophene cane limbs 2.  4 -Difluorene-N-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy- 2Η-cyclooctane [b] nanan-3 -Methyl) methyl] phenyl] -benzylamine 2,4.  β-trichloro-N-[3-[cyclopropyl (5, 6,7,8,9,1 0 -hexahydro-4 -Cycloyl-2 -oxy-2 -2 -cyclooctyl [b] piperazine Alan-3 -yl) methyl] phenyl] -benzylsulfonium [[^ [[^-[cyclopropyl ^ 彳 "^^^-hexahydro-fluorene-hydroxy · ^ -argonyl-2 -2- Cyclooctyl [b] piperan-3 -yl) methyl] phenyl] amino] sulfo-cyl] -Ethylamine printed by the Consumer Cooperatives of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the note on the back first) Please fill in this page again) Η-[3-[Cyclopropyl (5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 -2 -cyclooctyl [b] piperazine Nan-3-yl) methyl] cryl] -4- (phenylazo) -cylsulfonyl amine • N-"3-[cyclopropyl (5, β, 7, 8. 9,1 0 -hexahydro-4 -hydroxy-2 -oxy '-2Η-cyclooctyl [b] manan-3-yl) methyl] benzyl] -4-[[4- (dimethylformyl) $ Yl] Ethoxy] phenylcaryophyllamine N-[3-[cyclopropyl (5, 6,.  7, 8, 9, 1 0 -Hexahydro-4 -hydroxy-2 -oxy-9 5-This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) A8 B8 C8 D8 -2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (2-pyridyl) -2-fluorenylsulfonamide '• 3 -chloro-N- [3- [ Cyclopropyl (5,6,7,8,9,10 -Hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] B-Cetan-3-yl) methyl] phenyl]- 2-methylbenzoic acid amine N- [3- [cyclopropyl (5, 6, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 -cyclooctyl [b] Piperan-3-yl) methyl] phenyl] -4- (trifluoromethoxy) -benzenesulfonamide 3 -chloro-N- [3- [cyclopropyl (5,6, 7,8, 9, '10 -Hexahydro-4-hydroxy-2-oxolan-2H-cyclooctyl [b] lanan-3-yl) methyl] benzyl] -3-[(benzyl_yl) amino 1-propanesulfonamide hydrazone-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0 -hexaaza-4 -hydroxy- · 2-oxy-2 hydrazone -cyclooctyl [ b] piperan-3 -yl) methyl] phenyl] -3 -piperansulfonamide_N-[3-[cyclopropyl (5, β, 7,0 -hexahydro-4 -hydroxy-2- Oxy-2 fluorene-cyclooctyl [h] piperan-3 -yl) methyl] phenyl] -5 -methyl-3 -pyridinesulfonium_amine Central Ministry of Economic Affairs Prospective Employees' Consumer Cooperatives Seal I (谙 Please read the precautions on the back before filling this page) Η-[3-[cyclopropyl (5, 6, 7, 8, 9,, 10-hexahydro-4 -hydroxyl- 2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -ethenylsulfonamide N- [3- [cyclopropyl (5, β, 7,8, 9,10 -Hexahydro-4-hydroxy-2-oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] phenyl] -methanesulfonamide N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [h 1piperan-3 -yl) methyl] phenyl] -ethane Sulfonamide N- [3- [cyclopropyl (5,6,7,8; 9,10-hexahydro'-4-hydroxy-2-oxy-2 Η -cyclooctane [b 1piperan-3 -Methyl) Methyl] Cage base] Bensulfonylamine-97-This paper is made of Chinese National Standard (CNS) A4 (210X297 mm). This paper is printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs. A8 B8 C8 D8 Six 、 Application scope of patent N- [3- [cyclopropyl (5, 6, 73, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -2-phenyl-ethylenesulfonamide hydrazone- [3- [cyclopropyl (5, 6,7,8,9, 10 -hexahydro-4-hydroxy-2-oxy- 2 Η-cyclooctyl '[b] piperan-3 -yl) methyl] Benzyl] -benzylmethanamine H- [5-[[[3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy- 2-oxy-2 氧基-Cyclooctyl [b] piperan-3 -yl) methyl] fluorenyl] amino] sulfonyl] -4 -methyl-2-thienyl] -acetamidinium 'N-[3-[cyclo Propyl (5,6,7,8,9,1 0-hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] B olean-3 -yl) methyl] benzyl] -2 -thiophenesulfonamide-N-[3-[cyclopropane (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperazine Nan-3-yl) methyl] phenyl] -1-propanesulfonamide N- [3- [cyclopropyl (5, 6,7,8,9, 10-hexahydro-4-hydroxy-2- Oxy-2 fluorene-cyclooctyl [b] anan-3-yl) methyl] benzyl] -4-methyl-toluenesulfonamide 'N-[3-[cyclopropyl (5,6, 7 , 8,9,1 0 -Hexahydro-4 -Ethyl-2-oxy-2 fluorene, cyclooctyl [h] piperan-3 -yl) methyl] benzyl] -1 -butanesulfonamide N- [3- [cyclopropyl (5, R, 7, 8, 9, 10-hexahydro-4-hydroxyi2-oxy-2 氧基 -cyclooctyl [h] piperan-3 -yl) methyl ] Phenyl] -1,3-dihydro-U 3 -di_-2 Η-isoindole-2 -ethanesulfonamide Η-[3-[cyclopropyl (5, β; 7,8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctane [b 1 Alan-3 -yl) methyl] phenyl] -2-propanesulfonamide hydrazone-[3-[cyclopropyl (5, β, 7,8,9, 1 0 -hexahydro-4 -hydroxy-2 -Oxy-2 Η -cyclooctyl [h] piperan-3 -yl) methyl] phenyl] -2, Β-dimethylbenzenesulfonium m This paper is sized to Chinese National Standard (CNS> A4 Specification ( 210X297 mm) ft (please read the precautions on the back before filling this page) Order VI. Application scope of patent N- [3- [cyclopropyl (5, 6, 7,8,9,10-hexahydro-4 -Hydroxy-2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -2-methylbenzenesulfonamide 3- 醯-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-propanesulfon Amidine N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -3,5-bis (trifluoromethyl) -benzenesulfonyl-amine H- [3- [cyclopropyl (5,6,7,8,9,10-hexaargon-4- Hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -7,7-dimethyl-2-oxy-valent ring [2. 2. 1] Heptane-methanesulfonamide • Ν-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η- Cyclo [b] piperan-3 -yl) methyl] cagel] -2, β -dimethoxybenzenesulfonate-[3- [cyclopropyl (5, 6,7 9, 10- Hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b 1piperan-3 -yl) methyl] benzyl] -3,4-dimethoxy-benzyl hydrazone- [ 3- [cyclopropyl (5,6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl1) methyl] Phenyl] -3 -methyl-sulfenazamide printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 2-bromo-bu [3- [cyclopropyl (5 , 6,7,8,?), 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [blnanan-3-yl) methyl] phenyl] -β-methoxy-benzyl _Metamine-N- [3- [cyclopropyl (5, β, 7, S, 9,10-hexahydro-4 -hydroxy-2-oxy-2) -cyclooctyl [h] piperan- 3 -yl) Φ group] phenyl] -3, 5 -dimethyl-4 -Ishui beer sulfonyl gf amine-99-This paper size applies to Chinese national standard (CNS> A4g (210X297mm) A8 B8 C8 D8 Sixth, the scope of patent application 2-cyano-N- [3- [ring Propyl (5,6,7,8, 9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -benzenesulfonate Pickled • amine c N- [3- [cyclopropyl (5,6, 7, 8,9, 10 -hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3- (Methyl) methyl] phenyl] -2,1,3-benzoxadiazole-4 · -ammonium N- [3- [cyclopropyl (5, 6,7,8,9, 10 -hexa Hydrogen-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-ZΓ-benzenesulfonamide'H-[3-[cyclopropyl (5, β, 7, S, 9,1 0-hexahydro-4 -hydroxy-2 -oxy-2'-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4- Propyl-benzylsulfonamide N-[3-[cyclopropyl (5, 6,7, 8,9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b] Piperan-3 -yl) methyl] benzyl] -1 -octanesulfonamide N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1-dodecanesulfonamide H- [3- [cyclopropyl (5, β, 7, 8, 9 ,. 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -4-(1-methylethyl) -cagesulfonic mirror • H- [3- [Cyclopropylamidine (5. 6, 7,8,9, 10-Hexahydro-4-hydroxy-2-oxy Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) -2 Η-环 辛[b] Piran'-3 -yl] methyl] phenyl] -phenylethanesulfonamide N- [3- [cyclopropane (5, 6, 7,8,9, 10-hexahydro-4) -Hydroxy-2-oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] fluorenyl] -5-(3 -isomorphazolyl)-'2-fluorenylsulfonamide 4 -Amino-N- [3- [cyclopropyl (5, "), 7,8,9,10-hexahydro-4-hydroxy-2-chloro- 2H-cyclooctyl [b] piperan-3 -Methyl) methyl] phenyl] -benzylsulfonium [3- [cyclopropyl (5,6,7, S, 9,10-hexahydro-4-hydroxy-2-oxy-100-this paper The scale is applicable to Chinese National Standard (CNS) A4 specification (210X297 mm) ~ 6. Scope of patent application -2H-cyclooctyl [b] Xanan-3-yl) methyl] phenyl] -4- (hydroxylimyl) -Benzenesulfonamide N- [3- [cyclopropyl (5, 6, 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3 -Yl) methyl] phenyl] -4-[(phenylsulfonyl) amino] -benzoic acid amine H- [3-[cyclopropyl (5,6,7,8,9,10- Hexahydro-4-hydroxy-2 -oxy-2H -cyclooctyl [b] piperan-3-yl) methyl] benzene ] -3 - [(Ben vine sulfo group-yl) amino 1-- cage vine amine sulfonamide Ή - [3 - [[[3 - [cyclopropylmethyl. (5, β, 7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy -2Η -cyclooctyl [b] piperan-3-yl) methyl] phenyl] amino] Sulfuryl] Cagel] -benzyl-amine N- [3- [cyclopropyl (5,6,7,8, 9, 10-hexahydro- 4-rfyl-2-oxy-2 fluorene-ring Octyl [b] piperan-3 -yl] methyl] phenyl] -4-(dimethylamino) -benzyl 3 -aminopyrene-N-[3-[cyclopropyl (5, β, 7, 8, 9, 1 0 -Hexahydro-4 -hydroxy-2-oxy-2fluorene-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -benzenesulfonamide N-[3- [Cyclopropyl (5,6,7,8,9,1 0 -Hexahydro-4 -hydroxy-2 -oxy-2 "-cyclooctyl [b] piperan-3 -ylmethyl] phenyl] -3-(Hydroxy Saddle®) -Benzamide printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Please read the precautions on the back before filling this page) 3-[[[3- [cyclopropyl (5 , β, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenylhydrazine] amino] sulfonamide ] -Benzoic acid, methyl ester Η-[3-[cyclopropyl (5, R, 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctyl [b 1 Piperan-3 -yl) methyl] phenyl] -3-[(2-ethanol) amino-101-paper size A8 B8 C8 D8 six patented range] -s sulfonamide amine salt Falcon with China National Standard (CNS) A4 size (210X297 mm). N-[3-[cyclopropyl (5, 6,7, 8,9, 10-hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3-yl) Methyl] phenyl] -3- [bis- (2-ethanol)) aminobenzylsulfonamide N- [3-[cyclopropyl (5, 6,7,8,9, 10 -hexahydro- 4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -3- [methanol] -benzenesulfonamide N- [3- [cyclopropyl [ 3- (2-isothiazolidinyl) phenyl] methyl- (5,6,7,8,9,10-hexahydro-4 -hydroxy-S, S'-dioxide) methyl] benzyl Group] -3-[(phenylsulfonyl) amino] -4-2H-cyclooctyl [b] piperan-2- 嗣 N- [3- [cyclopropyl. (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] 5-octane-3-yl) methyl] phenyl] -3- ( 2-methoxyethoxymethoxybenzylamidine H- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 Fluorene-cyclooctyl [b] piperan-3-yl) fluorenyl] fluorenyl] -3 -hydroxy-benzenesulfonamide N-[3-[cyclopropyl (5, 6, 7, 8, 9, 9, 1 0 -Hexahydro-4 -Ethyl-2 -oxy-2H-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -3- (4-morpholineethoxy) _cage Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs of Bentomine (please read the precautions on the back before filling out this page) N-[3-[cyclopropyl (5, β, 7,8,9, 1 0 -six Hydrogen-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan-3 -yl) methyl] benzyl-3-(N, N -diethylaminoethoxy) -benzenesulfonate Tamine N- [3- [cyclopropyl (5, 6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) Methyl] fluorenyl] -4-hydroxy-benzenesulfonamide [3- [cyclopropyl (2,5, "), 7,8,9-hexahydro-4-hydroxy-2-fluorenylcycloheptan- 102-This paper size applies Chinese National Standard (CNS) A4 ^ grid (210X297 mm) ~~ A8 Λ Β8 8❹ 82_ __ VI. Application scope [b] piperan-3-yl) methyl] phenyl] -ethylenesulfonamide N- [3- [cyclopropyl (2,5,6,7,8,9-hexa Hydrogen-4-hydroxy-2-coppercyclohepta [b] piperan-3 -yl) methyl] phenyl] -methanesulfonamide ^ H- [3- [cyclopropyl (2, 5,6, 7 , 8,9-hexahydro-4-hydroxy-2- _cycloheptane [b] piperan-3-yl) methyl] phenyl] -ethanesulfonamide thiourea, N- [3- [cyclopropane (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [h] piperan-3-yl) methyl] phenyl] -N-benzene Basal gland, N-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctane-3 -Yl) methyl] phenyl] -N-ethyl-cetylthiopentamine, N- [3- [cyclopropyl (5, (5,7,8,9, 10-hexahydro-4- Hydroxy-2 -oxy-2 fluorene-cyclooctyl [b 1piperan-3 -yl) methyl] phenyl] -H7, 8, 9. 10 -hexahydro-4-hydroxy- 3- (1-¾ylbutyl) -2H-cyclooctyl "_ b] piperan_ 2-_. [3-[1- (5,6,7,8,9,10 -hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [h] piperan-3 -yl) -2-methyl Propyl] benzyl] -aminocarboxylic acid, phenyl methyl ester-3-[1-(3-aminophenyl) -2-methylpropyl] -5,6,7,8,9,1 0 -Hexamine-4 -Xingji-2Η _Huanxin [h] 呢喃 -2 -Printed by the Consumer Cooperatives of the Central Standardization Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 4-cyano 1- [3- [1-("), 7,8,9,10-hexahydro-4-hydroxy-2-oxy-2 Η -cyclooctyl [h] piperan-3 -yl) -2- Methylpropyl] rongyl] -toluidine-4-[-[- 7,8,9. 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) -2-methylpropyl] phenyl] -benzenesulfonamide hydrazone-[3-Π -(Γ), Γ).  7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2-cyclooctyl [b] piperan-3-yl)-2-methylpropyl 1-phenyl- 1 Η-Beerazole This paper size applies to Chinese National Standard (CNS) A4 specification (210X297 mm) 8 8 8 8 ABCD 386083 VI. Application for patent scope -4-Code brewing amine (Please read the notes on the back before filling in (This page) • [3-Π- (5,6,7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) butyl Phenyl] phenylaminocarboxylic acid, phenylmethyl ester 3- [1- (3-aminophenyl) butyl) -5,6,7,8,9,10-hexahydro-4-hydroxyl Gang- 2H -cyclooctyl [b] nanan-2-coppenazine, 4-ammonium-1 [3- [bu (5,6,7,8,9,10-hexahydro-4-hydroxy-2 -Oxy-2H-cyclooctyl [b] piperan-3-yl) butyl] phenyl. ] -Benzenesulfonamide, 4-cyano-N-[3-[1-(5, β, 7, 8, 9,] 0 -hexahydro-4-hydroxy-2-oxy-2 氧基 -cyclooctane [b] piperan-3-yl) butyl] phenyl] -3- (α-cyclopropylfluoren-2-ylmethyl) -4-hydroxy-5,6,7,8,9, fluorene .  0 -Hexahydrocyclooctyl [b] Nanan-2-one-3-(σ -ethylmethylphen-2-ylmethyl) -4 -hydroxy-5,6,7,8,9, 1 0 -hexahydro Cyclooctyl [h] piperan-2 -fluorene 3-(cr -ethyl (5-methylthiophene-2-ylmethyl) -4 -hydroxy-5, (5,7, 8,9. 10-Hexahydrocyclooctyl [丨 &gt;] Ninan-2-_ 3-(«-ethylbenzo [b] thiophene-2-ylmethyl) -4 -hydroxy-5, 6, 7, 8.  9,10-Hexahydrocyclooctyl [h] oxo-2-feed 3-U -cyclopropyl (5-hydroxymethylfuranmethyl-2 -yl) -4 -hydroxy -5, β · 7, 8. , 9, 10-Hexahydrocyclooctyl [b] Piperan-2-one, printed by the Consumer Cooperative of the Central Standards Bureau, Ministry of Economic Affairs, 3- («-Cyclopropyl (5-hydroxymethylthien-2-ylmethyl) ) -4-hydroxy-5, β, 7,8,9,10-hexahydrocyclooctyl [b] piperan-2 -b. 3-(«-cyclopropyl (5- (2-hydroxyethyl) thiophene-2-ylmethyl) -4-hydroxy-5, β, 7,8,9,19-hexahydrocyclooctyl [h] Naran-2- 嗣 3-(«-Cyclopropyl (5-(2 -Hydroxymethyl (methoxymethyl ether) furan-2--104-This paper size applies to Chinese National Standard (CNS) A4 specifications ( 210X: 297 mm) 386082 A8 B8 C8 D8 6. Scope of patent application (please read the notes on the back before filling this page) Base) -4 -hydroxy-5,6,7,8,9,10 -hexahydro Cyclooctane [b] piperan-2-_ 3- (α-cyclopropyl (5- (2-hydroxymethyl (methoxymethyl ether) thiophen-2-ylmethyl) -4 -hydroxy-5 , 6,7,8, 9, 10 -Hexahydrocyclooctyl [b] piperan-2-copper 3- (α-cyclopropyl (5-ΓΝ-benzyl ester) aminomethyl) furan-2- ) -4 -hydroxy-5, Γ), 7, δ, 9,10-Hexahydrocyclooctyl [b] piperan-2-one-3U-cyclopropyl (5-ΓN-benzyl ester group) Aminemethyl) thien-2-ylmethyl) -4 -hydroxy-5, Γ), 7, 8, 9, 10 -hexahydrocyclooctyl [b] piperan-2-嗣 K-[3-[ Cyclopropyl (5, (5, 7, 8, 9, 9, 10-hexahydro-4 -hydroxy-2 -oxy-2H-cyclooctyl [b] piperan-3- 棊) methyl] furanmethyl- 2-ylmethyl] 4-fluorobenzene Hydrazine_N-[3-[cyclopropyl (5, Γ), 7,8,9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 fluorene -cyclooctyl [b] piperan- 3 -yl) methyl] furan-2-ylmethyl] 4-cyanobenzylsulfonium-amine N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro -4-Hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] methylphen-2-2-ylmethyl'yl] 4-cyanobenzidine K- [3- [cyclopropyl (5, β, 7,8,9,10-hexahydro-4 -hydroxy-2-oxy-2Η-cyclooctyl [b] piperan- 3 -yl) Φ group] thiophen-2-ylmethyl] 4-cyanobenzenesulfonylamine-cyclopropyl (5-methyl-4-hydroxymethylthiophen-2-ylmethyl) -4 -hydroxy -5, β, 7,8,9,1 0 -Hexahydrocyclooctyl [b] piperan-2-one-3U [S] -ethylbenzyl) -4 -hydroxy-5, "), 7 , 8, 9,10-hexahydrocyclooctane [b] Piran-2-'嗣 -105-This paper size applies to Chinese National Standard (CNS) A4 ^ (210X297 mm) A8 38β〇82 D8 VI. Application Patent scope 3- (σ U) -ethylbenzyl) -4-hydroxy-5,6,7,8,9,10-hexahydrocyclooctyl [b] nanan-2-one N- [3- [cyclo Propyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxy-2H-ring Octyl [b] piperan-3-yl) methyl] phenyl] phenylamine sulfate ^-[3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -N, N -dimethylthiosulfamine N-[3-[cyclopropyl (5, 6 , 7, 8, 9, 10-hexahydro-4-hydroxy-2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] benzyl] -4-methyl-buhexahydro Pycnogenol's saddle '______ H -cagel-3- [cyclopropyl (5, Γ), 7, 8,9, 10 -hexahydro-4-hydroxy-2-oxy-2 Η -cyclooctyl [ b] piperan-3 -yl) methyl] -benzenesulfonamide N-[3- [cyclopropyl (5, Γ), 7, 8,9,10 -hexahydro-4-hydroxy-2-oxo -2 hydrazone-cyclooctyl [h] piperan-3-yl) methyl] phenyl- (R) -benzenesulfenamine 4-cyano-N- [3- [cyclopropyl (5,6, 7,8,9,10-hexahydro-4- mesityl-2-oxy-2'-cyclooctyl [b] mannan-3-yl) methyl] phenyl] -bentolide. N-[3-[cyclopropyl (5, Γ), 7, 8, 9, 1 0 -hexahydro-4 -hydroxy-2 -oxy-2 Η -cyclooctane [h 1piperan-3 -yl ) Methyl] phenyl]-'4-(Dimethylanyl Y benzene sulfonate brewed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) 4-(Bromomethyl ) -N-[3-[Cyclopropyl (5,6,7,8,9,10 -Hexahydro-4 -hydroxy-2 -oxy-2H -cyclooctyl [b] anan-3-yl ) Methyl] phenyl] -benzyl rattan saddle 4-[[[3- [cyclopropyl (5, 6, 7, 8,9,10-hexahydro-4-hydroxy-2-oxy-2 Η -Cyclooctyl [b] mairan-3 -yl) methyl] phenyl] amino] • sulfonyl] -benzylidene--106-This paper size applies to Chinese National Standard (CNS> A4 Specification (210X297) (%) A8 386082 1 Uo 6. Scope of patent application (please read the notes on the back before filling this page) M- [3- [cyclopropyl (5,6, 7,8,9,10-hexahydro- 4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3-yl) methyl] phenyl] -5- (phenylsulfonyl)-, (S) _2-Hipene Benzene amine H- [3-[cyclopropyl (5, Γ), 7,8,9,10 -hexahydro-4-hydroxy-2 -oxy-2 Η -cyclooctane [b] nanan-3- Methyl)] Yl] -3 - hydroxy - benzenesulfonamide vine amine.   N- [3- [cyclopropyl (5, β, 7, 8,9, 10-hexahydro-4-hydroxy-2-oxy-2 fluorene-cyclooctyl [b] piperan-3 -yl) formyl Phenyl] phenyl] -4-fluoro-benzenesulfonamide 4-Toxy-N- [3- [cyclopropyl (5, "), 7,8,9,10-hexahydro-4-hydroxy- 2-oxy-2H-cyclooctyl [b] piperan-3-yl) methyl] phenyl] benzenesulfonamide 5 -fluorene-N-[3-[cyclopropyl (5, β, 7,8 , 9,1 0 -hexahydro-4 -hydroxy-2 -oxy-2 2 -cyclooctyl [b] piperan-3-yl) methyl] phenyl] -1,3-dimethyl-1 -1 _ 1% beer_ 4-lutenamine 2,4-dihydrazine-N- [3- [cyclopropyl (5,6,7,8,9,10-hexahydro-4-hydroxy-2-hydroxyl -2Η-cyclooctyl [b] nickan-3-yl) methyl] benzyl] benzamide N- [3- [cyclopropyl (5, β, 7, 8, 9, 10-hexahydro- 4-hydroxy-2-oxy.   -2 Η -cyclooctyl [b] piperan-3 -yl) methyl] fluorenyl] -4 -hydroxy-benzenesulfonamide -10 -10 7-This paper uses China National Standard (CNS) A4 (210X297 mm) ~~